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> AZD5582 [1258392-53-8]

AZD5582 [1258392-53-8]

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Cat# HY-12600-10mg

Size : 10mg

Brand : MedChemExpress

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Description

AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis[1].

IC50 & Target[1]

cIAP1

15 nM (IC50)

cIAP2

21 nM (IC50)

XIAP

15 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 GI50
< 0.06 nM
Compound: 14, AZD5582
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay
[PMID: 24320998]
MDA-MB-231 EC50
0.1 nM
Compound: 14, AZD5582
Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA
Binding affinity to cIAP1 in human MDA-MB-231 cells assessed as induction of protein degradation after 1 hr by ELISA
[PMID: 24320998]
In Vitro

AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[2].
AZD5582 (20 nM; 17 or 25 hours) downregulates cIAP-1, activates RIPK1 (upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7[2].
AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells[2].

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

AZD5582 Related Antibodies

Cell Viability Assay[2]

Cell Line: H1975 NSCLC cell line
Concentration: 20 nM
Incubation Time: 48 hours
Result: Cooperated with IFNγ or viral double-stranded RNA (dsRNA) to inhibit cell viability even cell death.

Apoptosis Analysis[2]

Cell Line: HCC827 NSCLC cell line
Concentration: 20 nM
Incubation Time: 48 hours
Result: Had an inhibitory effect on cell viability by cooperating with IFNγ.

Western Blot Analysis[2]

Cell Line: H1975 NSCLC cell line
Concentration: 20 nM
Incubation Time: 17 or 25 hours
Result: Down-regulated cIAP-1, activated RIPK1 (upstream regulator of caspase-8), triggered the cleavage (activation) of caspase-3,7,8 and 9.
In Vivo

AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved; when the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect[1].

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

Animal Model: MDA-MB-231 xenograft-bearing mice[1]
Dosage: 0.1 mg/kg, 0.5 mg/kg, 3.0 mg/kg
Administration: Intravenous injection; once a week; 2 weeks
Result: Resulted in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg
Molecular Weight

1015.29

Formula

C58H78N8O8
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CN[C@@H](C)C(N[C@H](C(N1[C@H](C(N[C@H]2C3=CC=CC=C3C[C@H]2OCC#CC#CCO[C@H]4[C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@H](C)NC)=O)C6CCCCC6)=O)=O)C(C=CC=C7)=C7C4)=O)CCC1)=O)C8CCCCC8)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (98.49 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 0.9849 mL 4.9247 mL 9.8494 mL
5 mM 0.1970 mL 0.9849 mL 1.9699 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, stored under nitrogen). 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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.46 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.46 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 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.

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:  50% PEG300    50% Saline

    Solubility: 50 mg/mL (49.25 mM); Clear solution; Need ultrasonic
Purity & Documentation
References

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