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

Fludarabine [21679-14-1]

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Cat# HY-B0069-5mg

Size : 5mg

Brand : MedChemExpress

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Description

Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes^[1]^[2]^[3]^[4].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	47.44 μM Compound: fludarabine	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 20605656]
CCRF-CEM	IC₅₀	19.49 μM Compound: fludarabine	Cytotoxicity against human CEM cells after 72 hrs by MTT assay Cytotoxicity against human CEM cells after 72 hrs by MTT assay	[PMID: 20605656]
HCT-116	IC₅₀	6.6 μM Compound: Fludarabine	Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 25462277]
HCT-116	IC₅₀	8 μM Compound: Fludarabine	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay	[PMID: 29326016]
HeLa	EC₅₀	16 μM Compound: Flu	Antitumor activity against human HeLa cells assessed as cell viability by MTT assay Antitumor activity against human HeLa cells assessed as cell viability by MTT assay	[PMID: 24673739]
HepG2	IC₅₀	20 μM Compound: Fludarabine	Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay	[PMID: 29326016]
Huh-7	IC₅₀	30 μM Compound: Fludarabine	Antiproliferative activity against human HuH7 cells after 72 hrs by SRB assay Antiproliferative activity against human HuH7 cells after 72 hrs by SRB assay	[PMID: 29326016]
Huh-7	IC₅₀	60.1 μM Compound: Fludarabine	Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay	[PMID: 25462277]
JVM-2	EC₅₀	10.4 μM Compound: Flu	Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis	[PMID: 24673739]
K562	IC₅₀	0.26 μM Compound: fludarabine	Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay	[PMID: 20605656]
K562	IC₅₀	0.6 μg/mL Compound: Fludarabine	Inhibitory concentration required against human chronic myelogenous leukemic K-562 cell line after 48h, using [3H]thymidine incorporation assay Inhibitory concentration required against human chronic myelogenous leukemic K-562 cell line after 48h, using [3H]thymidine incorporation assay	[PMID: 12617912]
K562	IC₅₀	0.6 μg/mL Compound: Fludarabine	Inhibitory concentration required against human chronic myelogenous leukemic K-562 cell line after 5h, using [3H]thymidine incorporation assay Inhibitory concentration required against human chronic myelogenous leukemic K-562 cell line after 5h, using [3H]thymidine incorporation assay	[PMID: 12617912]
K562	IC₅₀	267 μM Compound: fludarabine	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 20605656]
Mahlavu	IC₅₀	10 μM Compound: Fludarabine	Antiproliferative activity against human Mahlavu cells after 72 hrs by SRB assay Antiproliferative activity against human Mahlavu cells after 72 hrs by SRB assay	[PMID: 29326016]
MCF7	IC₅₀	15 μM Compound: Fludarabine	Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay	[PMID: 29326016]
PBMC	IC₅₀	1.9 μM Compound: fludarabine	Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay	[PMID: 25562417]
PBMC	IC₅₀	10 μM Compound: fludarabine	Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay in presenc of mouse M210B4 cells Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay in presenc of mouse M210B4 cells	[PMID: 25562417]
PBMC	IC₅₀	14 μM Compound: fludarabine	Cytotoxicity against healthy human PBMC after 48 hrs by CellTitre-Blue assay Cytotoxicity against healthy human PBMC after 48 hrs by CellTitre-Blue assay	[PMID: 25562417]
T47D	IC₅₀	46.2 μM Compound: Fludarabine	Cytotoxicity against human T47D cells after 72 hrs by SRB assay Cytotoxicity against human T47D cells after 72 hrs by SRB assay	[PMID: 25462277]

In Vitro

Fludarabine (5 μM; 48 hours) induces a decrease in p27kip1 expression^[4].

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

Western Blot Analysis^[4]

Cell Line:	B-CLL cells
Concentration:	5 μM
Incubation Time:	24 hours
Result:	Induces a decrease in p27kip1 expression. The decrease in p27kip1 expression was significantly correlated to the extent of in vitro apoptosis.

In Vivo

Fludarabine (0.8 mg/kg; i.p.; two cycles for 5 days every 2 weeks) in combination with Cyclophosphamide (400 mg/kg; i.p.; 2 weeks) decreases incidence of GVHD^[6].

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

Animal Model:	F-1 mice received 105 BCL-1 leukemia cells^[6]
Dosage:	0.8 mg/kg
Administration:	Intraperitoneal injection; two cycles for 5 days every 2 weeks
Result:	Combination with Cyclophosphamide decreased incidence of graft-versus-host disease (GVHD).

Clinical Trial

Molecular Weight

285.24

Formula

C₁₀H₁₂FN₅O₄

CAS No.

21679-14-1

Appearance

Solid

Color

White to yellow

SMILES

O[C@H]1[C@H](O)[C@H](N2C(N=C(F)N=C3N)=C3N=C2)O[C@@H]1CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (87.65 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	3.5058 mL	17.5291 mL	35.0582 mL
5 mM	0.7012 mL	3.5058 mL	7.0116 mL
10 mM	0.3506 mL	1.7529 mL	3.5058 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. 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 (8.76 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 (8.76 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.76 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: 50% PEG300 50% Saline
Solubility: 5 mg/mL (17.53 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.85%

Data Sheet (282 KB) SDS (393 KB)

COA (253 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Liang YB, et al. Downregulated SOCS1 expression activates the JAK1/STAT1 pathway and promotes polarization of macrophages into M1 type. Mol Med Rep. 2017 Nov;16(5):6405-6411. [Content Brief]

[2]. Sanhes L, et al. Fludarabine-induced apoptosis of B chronic lymphocytic leukemia cells includes early cleavage of p27kip1 by caspases. Leukemia. 2003 Jun;17(6):1104-11. [Content Brief]

[3]. Frank DA, et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999;5(4):444-447. [Content Brief]

[4]. Frank DA,et al. Fludarabine-induced immunosuppression is associated with inhibition of STAT1 signaling. Nat Med. 1999 Apr;5(4):444-7. [Content Brief]

[5]. Tournilhac O, et al. Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11. [Content Brief]

[6]. Weiss L, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintainseffective graft-versus-leukemia effect after allogeneic stem cell transplantation in murinelymphocytic leukemia. Bone Marrow Transplant. 2003 Jan;31(1):11-5. [Content Brief]

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