Reagents and instruments for immunology, cell biology and molecular biology.

Ibrutinib [936563-96-1]

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Cat# HY-10997-50mg

Size : 50mg

Brand : MedChemExpress

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Description

Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM^[1].

IC₅₀ & Target

IC50: 0.5 nM (Btk)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	EC₅₀	20.1 μM Compound: ibrutinib	Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human A2780 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
A-431	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human A431 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
A-431	EC₅₀	2.38 μM Compound: Ibrutinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A549 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
A549	IC₅₀	21.79 μM Compound: Ibrutinib	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 28734581]
B cell	IC₅₀	8 nM Compound: 19	Antiproliferative activity against anti-IgM-stimulated human KB cells assessed as cell growth inhibition pretreated for 30 mins followed by anti-IgM stimulation for 72 hrs by celltiter-glo reagent based assay Antiproliferative activity against anti-IgM-stimulated human KB cells assessed as cell growth inhibition pretreated for 30 mins followed by anti-IgM stimulation for 72 hrs by celltiter-glo reagent based assay	[PMID: 33540357]
BaF3	IC₅₀	> 1 μM Compound: 7	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	GI₅₀	> 10 μM Compound: 1; PCI-32765	Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay Cytotoxicity against mouse BAF3 cells assessed as cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	> 10 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
BaF3	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
BaF3	GI₅₀	> 10 μM Compound: 9; PCI-32765	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	GI₅₀	0.12 μM Compound: 1; PCI-32765	Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay Inhibition of FLT3 ITD mutant (unknown origin) expressed in BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
BaF3	GI₅₀	0.12 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
BaF3	GI₅₀	2.5 μM Compound: 9	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutation after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-F691L mutation after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
CMK	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human CMK cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human CMK cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
DOHH-2	IC₅₀	0.023 μM Compound: Ibrutinib	Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 35247756]
DOHH-2	IC₅₀	0.0334 μM Compound: Ibrutinib	Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human DOHH2 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30522954]
DOHH-2	GI₅₀	0.41 μM Compound: Ibrutinib	Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human DOHH2 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
DOHH-2	IC₅₀	0.5062 μM Compound: Ibrutinib	Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
DU-145	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human DU145 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human DU145 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
DU-145	IC₅₀	2 μM Compound: Ibrutinib	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
Granta-519	IC₅₀	9.7 μM Compound: IBN	Antiproliferative activity against human GRANTA-519 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human GRANTA-519 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
HCC 2998	IC₅₀	15.85 μM Compound: Ibrutinib	Antiproliferative activity against human HCC 2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HCC 2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
HCC827	IC₅₀	0.039 μM Compound: Ibrutinib	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant after 72 hrs by MTT assay	[PMID: 28734581]
HCC827	EC₅₀	0.45 μM Compound: Ibrutinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCT-116	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT116 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HEK293	IC₅₀	19.3 μM Compound: Ibrutinib	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
HEK293	IC₅₀	46.7 nM Compound: 1a	Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay Inhibition of TEC phosphorylation in HEK293 cells peincubated for 3 hrs followed by pervanadate stimulation and measured after 20 mins by MSD assay	[PMID: 31381333]
HEK293	IC₅₀	7.9 μM Compound: ibrutinib	Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells	[PMID: 35163125]
HEK-293T	IC₅₀	0.9 μM Compound: Ibrutinib	Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay Inhibition of PF-06658607 binding to recombinant C-terminal FLAG-tagged FAM213A (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay	[PMID: 28280261]
HEL	IC₅₀	> 20 μM Compound: Ibrutinib	Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
HEL	GI₅₀	4 μM Compound: 1; PCI-32765	Antiproliferative activity against human HEL cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HEL cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HeLa	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human HeLa cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HeLa cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HeLa	IC₅₀	16.8 μM Compound: ibrutinib	Cytotoxicity against human HeLa cells expressing GFP assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human HeLa cells expressing GFP assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
HL-60	GI₅₀	3.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HL60 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
HL-60	IC₅₀	3.57 μM Compound: Ibrutinib	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30881616]
HL-60	IC₅₀	8 μM Compound: Ibrutinib	Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay	[PMID: 30077608]
HL-60(TB)	IC₅₀	19.95 μM Compound: Ibrutinib	Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
HT	GI₅₀	15.9 μM Compound: Ibrutinib	Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay Antiproliferative activity against human HT cells measured after 72 hrs by calcein AM dye-based fluorescence assay	[PMID: 30943029]
JeKo-1	IC₅₀	1.1 μM Compound: 24	Antiproliferative activity against human JeKo-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human JeKo-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]
JeKo-1	IC₅₀	1.5 μM Compound: IBN	Antiproliferative activity against human JeKo1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human JeKo1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
JeKo-1	IC₅₀	20 μM Compound: IBN	Antiproliferative activity against human resistant Jeko cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human resistant Jeko cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
JeKo-1	IC₅₀	207.47 nM Compound: Ibrutinib	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
JeKo-1	IC₅₀	3 μM Compound: Ibrutinib	Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
JeKo-1	IC₅₀	330.2 nM Compound: Ibrutinib	Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
Jurkat	IC₅₀	76.9 nM Compound: 1a	Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis Inhibition of ITK in human Jurkat cells assessed as reduction in PLCgamma1 phosphorylation at Y783 residues preincubated for 2 hrs followed by H2O2 addition and measured after 10 mins by Western blot analysis	[PMID: 31381333]
JVM-2	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human JVM2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
K562	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
K562	IC₅₀	7.5 μM Compound: Ibrutinib	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30077608]
L02	IC₅₀	17.4 μM Compound: Ibrutinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
LNCaP C4-2	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human C4-2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human C4-2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Maver1	IC₅₀	10.4 μM Compound: IBN	Antiproliferative activity against human Maver1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Maver1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Maver1	IC₅₀	14.4 μM Compound: IBN	Antiproliferative activity against human Maver1 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human Maver1 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
Maver1	IC₅₀	7.8 μM Compound: 24	Antiproliferative activity against human MAVER-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human MAVER-1 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]
MDA-MB-468	IC₅₀	0.03 μM Compound: Ibrutinib	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
MIA PaCa-2	IC₅₀	16.6 μM Compound: ibrutinib	Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human MIAPaCa2 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
MM1.S	IC₅₀	> 20000 nM Compound: Ibrutinib	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
MOLM-13	GI₅₀	1.3 μM Compound: 1; PCI-32765	Antiproliferative activity against human MOLM13 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM13 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
MOLM-14	GI₅₀	1.8 μM Compound: 1; PCI-32765	Antiproliferative activity against human MOLM14 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
MOLT-4	IC₅₀	3.98 μM Compound: Ibrutinib	Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
MV4-11	GI₅₀	0.33 μM Compound: 1; PCI-32765	Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CelltiterGlo assay	[PMID: 26630553]
MV4-11	GI₅₀	0.33 μM Compound: 9	Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28956923]
NALM-6	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NALM6 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NALM6 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NAMALVA	IC₅₀	10.45 μM Compound: Ibrutinib	Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
NAMALVA	IC₅₀	19.6 μM Compound: Ibrutinib	Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK8 assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK8 assay	[PMID: 30006143]
NAMALVA	GI₅₀	6 μM Compound: 1; PCI-32765	Antiproliferative activity against human NAMALWA cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NB-4	GI₅₀	7.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human NB4 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NB4 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H1975	EC₅₀	0.64 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	GI₅₀	1.2 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H1975	IC₅₀	1.27 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 28734581]
NCI-H322M	IC₅₀	0.1 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H322M cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
NCI-H358	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H358 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H358 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H460	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NCI-H460 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
NCI-H522	IC₅₀	0.06 μM Compound: Ibrutinib	Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human NCI-H522 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
NOMO-1	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human NOMO1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human NOMO1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-AML2	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-AML-3	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
OCI-Ly10	IC₅₀	0.3 nM Compound: 1a	Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay Antiproliferative activity against human OCI-LY10 cells after 6 days by Celltiter-glo luminescent cell viability assay	[PMID: 31381333]
OCI-Ly10	IC₅₀	1 μM Compound: Ibrutinib	Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
OCI-Ly10	IC₅₀	1030 nM Compound: Ibrutinib	Antiproliferative activity against human OCILY10 cells harboring BTK C481S mutant knockout gene assessed as reduction in cell viability after 96 hrs Antiproliferative activity against human OCILY10 cells harboring BTK C481S mutant knockout gene assessed as reduction in cell viability after 96 hrs	[PMID: 34529443]
OCI-Ly10	IC₅₀	2.29 nM Compound: Ibrutinib	Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
OCI-Ly3	IC₅₀	> 10 μM Compound: Ibrutinib	Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human OCILY3 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
OVCAR-4	IC₅₀	7.94 μM Compound: Ibrutinib	Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
Pfeiffer	GI₅₀	0.002 μM Compound: Ibrutinib	Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human Pfeiffer cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Pfeiffer	IC₅₀	1.652 μM Compound: Ibrutinib	Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Pfeiffer	GI₅₀	8.4 μM Compound: 1; PCI-32765	Antiproliferative activity against human Pfeiffer cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Raji	IC₅₀	> 10 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Raji cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Raji	IC₅₀	> 20 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Raji	IC₅₀	1.49 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30522954]
Raji	IC₅₀	1.49 μM Compound: 1	Antiproliferative activity against human Raji cells after 48 hrs by CCK8-based assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8-based assay	[PMID: 29567295]
Raji	IC₅₀	12.56 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 32402933]
Raji	IC₅₀	14.2 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30077608]
Raji	IC₅₀	14.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Raji	IC₅₀	14.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by MTT assay Antiproliferative activity against human Raji cells after 48 hrs by MTT assay	[PMID: 30881616]
Raji	IC₅₀	15.2 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Raji	IC₅₀	15.99 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells measured after 72 hrs by CCK-8 assay	[PMID: 31234030]
Raji	IC₅₀	17.7 μM Compound: 1	Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Raji	IC₅₀	19.3 μM Compound: 1	Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Raji	IC₅₀	19.3 μM Compound: 1	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Raji	IC₅₀	19.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Raji	IC₅₀	19.5 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 72 hrs by CCK8 assay Antiproliferative activity against human Raji cells after 72 hrs by CCK8 assay	[PMID: 30006143]
Raji	IC₅₀	20.88 μM Compound: Ibrutinib	Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Ramos	IC₅₀	> 7.5 nM Compound: Ibrutinib	Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis	[PMID: 24915291]
Ramos	IC₅₀	0.5 nM Compound: Ibrutinib	Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay Inhibition of PF-06658607 binding to BTK in human Ramos cells after 1 hr by gel-based ABPP assay	[PMID: 28280261]
Ramos	IC₅₀	0.92 μM Compound: 1; PCI-32765	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 29715023]
Ramos	IC₅₀	1.35 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 32402933]
Ramos	IC₅₀	1.88 μM Compound: 1	Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Ramos	IC₅₀	12.6 μM Compound: 1	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Ramos	IC₅₀	14 nM Compound: Ibrutinib	Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis	[PMID: 24915291]
Ramos	IC₅₀	14 nM Compound: 1a	Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec Inhibition of BTK in human Ramos B cells assessed as reduction in BCR-stimulated calcium flux after 1 hr in dark condition measured for 180 sec	[PMID: 30893553]
Ramos	IC₅₀	14.69 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells measured after 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells measured after 72 hrs by CCK-8 assay	[PMID: 31234030]
Ramos	IC₅₀	2.088 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Ramos cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Ramos	IC₅₀	2.31 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by MTT assay Antiproliferative activity against human Ramos cells after 48 hrs by MTT assay	[PMID: 30881616]
Ramos	IC₅₀	2.4 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Ramos	IC₅₀	28.7 μM Compound: Ibrutinib	Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay	[PMID: 28274675]
Ramos	IC₅₀	3.5 nM Compound: 1a	Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay Inhibition of BTK in human Ramos cells assessed as reduction in BTK phosphorylation at Tyr223 residue preincubated for 1 hr followed by pervanadate or Na3VO4 stimulation for 20 mins by HTRF assay	[PMID: 31381333]
Ramos	GI₅₀	3.9 μM Compound: 1; PCI-32765	Antiproliferative activity against human Ramos cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Ramos cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Ramos	IC₅₀	5.14 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Ramos	IC₅₀	5.14 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 72 hrs by CCK8 assay	[PMID: 30006143]
Ramos	IC₅₀	5.8 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30605829]
Ramos	IC₅₀	5.88 μM Compound: 1	Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Ramos	IC₅₀	6.18 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 30108960]
Ramos	IC₅₀	6.62 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Ramos	IC₅₀	6.66 μM Compound: PCI-32765	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31221612]
Ramos	IC₅₀	8.11 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Ramos	IC₅₀	8.26 μM Compound: Ibrutinib	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8 assay	[PMID: 30522954]
Ramos	IC₅₀	8.26 μM Compound: 1	Antiproliferative activity against human Ramos cells after 48 hrs by CCK8-based assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK8-based assay	[PMID: 29567295]
Rec1	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human Rec1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Rec1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Rec1	IC₅₀	0.0008 μM Compound: Ibrutinib	Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human REC1 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
Rec1	IC₅₀	1.1 μM Compound: IBN	Antiproliferative activity against human Rec1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Rec1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Sf9	IC₅₀	> 25 μM Compound: Ibrutinib	Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP	[PMID: 30943029]
Sf9	IC₅₀	0.0018 μM Compound: Ibrutinib	Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of human recombinant full length N-terminal His tagged BTK expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31234030]
Sf9	IC₅₀	0.017 μM Compound: Ibrutinib	Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of human recombinant full length N-terminal His tagged BTK C481S mutant expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate measured after 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31234030]
Sf9	IC₅₀	0.3 nM Compound: Ibrutinib	Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay	[PMID: 27994736]
Sf9	IC₅₀	0.34 nM Compound: Ibrutinib	Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay	[PMID: 27956037]
Sf9	IC₅₀	0.5 nM Compound: PCI-32765	Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate after 60 mins by TR-FRET Assay	[PMID: 21958547]
Sf9	IC₅₀	16.1 nM Compound: Ibrutinib	Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31866272]
Sf9	IC₅₀	200 nM Compound: PCI-32765	Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay Inhibition of LYN-A expressed in Sf9 cells after 60 mins by TR-FRET Assay	[PMID: 21958547]
Sf9	IC₅₀	3.4 nM Compound: 1	Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay Inhibition of full-length human C-terminal His6-tagged BTK C481S mutant expressed in Sf9 insect cells using FAM-Srctide peptide as substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET Lanthascreen assay	[PMID: 30655951]
Sf9	IC₅₀	3.89 nM Compound: 1	Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay	[PMID: 31395509]
SKM-1	GI₅₀	3.9 μM Compound: 1; PCI-32765	Antiproliferative activity against human SKM1 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SKM1 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
SK-MEL-5	IC₅₀	6.31 μM Compound: Ibrutinib	Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
SNB-75	IC₅₀	3.16 μM Compound: Ibrutinib	Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
SUD4	IC₅₀	0.804 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SU-DHL-2	GI₅₀	2.2 μM Compound: 1; PCI-32765	Antiproliferative activity against human SUDHL2 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SUDHL2 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
SU-DHL-6	GI₅₀	0.58 μM Compound: Ibrutinib	Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human SU-DHL6 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
SU-DHL-6	IC₅₀	0.8742 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30522954]
SU-DHL-6	IC₅₀	1.498 μM Compound: Ibrutinib	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
SW480	IC₅₀	25.6 μM Compound: ibrutinib	Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 3 days by presto blue dye based plate reader method	[PMID: 27077228]
THP-1	IC₅₀	20.1 μM Compound: Ibrutinib	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 29324347]
TMD8	IC₅₀	0.01 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 33740548]
TMD8	IC₅₀	0.01 μM Compound: PCI-32765	Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human TMD8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31221612]
TMD8	IC₅₀	0.01 μM Compound: 1; PCI-32765	Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay Antiproliferative activity against human TMD8 cells after 72 hrs by MTT assay	[PMID: 29715023]
TMD8	IC₅₀	2.7 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human TMD8 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 35939993]
TMD8	IC₅₀	6.4 nM Compound: Ibrutinib	Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay	[PMID: 35671249]
U-251	IC₅₀	6.31 μM Compound: Ibrutinib	Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human U-251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
U2932	GI₅₀	4 μM Compound: 1; PCI-32765	Antiproliferative activity against human U2932 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human U2932 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
U-937	IC₅₀	4.4 μM Compound: 1; PCI-32765	Antiproliferative activity against human U-937 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-937 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 35099969]
U-937	GI₅₀	8.5 μM Compound: 1; PCI-32765	Antiproliferative activity against human U937 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human U937 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
UO-31	IC₅₀	1.26 μM Compound: Ibrutinib	Antiproliferative activity against human UO-31 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human UO-31 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 34237622]
WSU-NHL	GI₅₀	1.09 μM Compound: Ibrutinib	Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human WSU-NHL cells assessed as growth inhibition after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 24915291]
Z-138	GI₅₀	> 10 μM Compound: 1; PCI-32765	Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Z138 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28628824]
Z-138	IC₅₀	11.3 μM Compound: IBN	Antiproliferative activity against human Z138 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay Antiproliferative activity against human Z138 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell-titer-Glo luminescent cell viability assay	[PMID: 30857748]
Z-138	IC₅₀	14.4 μM Compound: IBN	Antiproliferative activity against human Z138 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human Z138 cells assessed as reduction in viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 31229421]
Z-138	IC₅₀	9.7 nM Compound: 24	Antiproliferative activity against human Z138 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Z138 cells assessed as reduction cell viability measured after 24 hrs by Cell Titer-Glo Luminescent Cell Viability Assay	[PMID: 36324498]

In Vitro

Ibrutinib (PCI-32765) selectively inhibits B-cell signaling and activation. It inhibits autophosphorylation of Btk (IC₅₀=11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC₅₀=29 nM), and phosphorylation of a further downstream kinase, ERK (IC₅₀=13 nM)^[1].
Ibrutinib (PCI-32765) inhibits BCR-activated primary B cell proliferation (IC₅₀=8 nM). Following FcγR stimulation, Ibrutinib (PCI-32765) inhibits TNFα, IL-1β and IL-6 production in primary monocytes (IC₅₀=2.6, 0.5, 3.9 nM, respectively)^[3].
Ibrutinib binds C481 (Cysteine481) of BTK with an ideal IC₅₀ of 0.5?nM. Ibrutinib cannot form a covalent bond with the hydroxyl group of serine, C481S mutation increases the IC₅₀ against BTK-C481S phosphorylation from 2.2?nM to 1?μM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (227.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2701 mL	11.3507 mL	22.7015 mL
5 mM	0.4540 mL	2.2701 mL	4.5403 mL
10 mM	0.2270 mL	1.1351 mL	2.2701 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (6.24 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.68 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 3.33 mg/mL (7.56 mM); Suspension solution; Need ultrasonic

Purity & Documentation

Purity: 99.97%

Data Sheet (285 KB) SDS (393 KB)

COA (257 KB) LCMS (93 KB) Elemental Analysis Report (114 KB)

Handling Instructions (2659 KB)

References

[1]. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. [Content Brief]

[2]. Herman SE, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011 Jun 9;117(23):6287-96. [Content Brief]

[3]. Chang BY, et al. The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells. Arthritis Res Ther. 2011 Jul 13;13(4):R115. [Content Brief]

[4]. Sun Y, et al. PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies. Cell Res. 2018 Jul;28(7):779-781. [Content Brief]

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