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  2. Bcl-2 Family
  3. A-385358

A-385358 

Cat. No.: HY-16014 Purity: 99.05%
Handling Instructions

A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.

For research use only. We do not sell to patients.

A-385358 Chemical Structure

A-385358 Chemical Structure

CAS No. : 406228-55-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 493 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.

IC50 & Target[1]

Bcl-xL

0.8 nM (Ki)

Bcl-2

67 nM (Ki)

In Vitro

A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-XL cells for 24 hours with A-385358 results in cell killing with an EC50 of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-XL versus Bcl-2 hydrophobic grooves, the EC50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-XL cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-XL versus Bcl-2 cells[1].

In Vivo

The combination of A-385358 given at 100 mg/kg/d plus the lower dose of paclitaxel produces a significant reduction in tumor growth (%T/C) compare with paclitaxel monotherapy. This combination also yields a >100% increase in time for tumors to reach 900 mm3 (%ILS) compare with vehicle control. Maximal efficacy is observed during the dosing period for A-385358, with slow but steady increase in the tumor growth after termination of treatment. The combination of A-385358 at 75 mg/kg/d plus paclitaxel at 30 mg/kg/d is also well tolerated and inhibits tumor growth rate by nearly 80%. Significant effects on tumor growth relative to paclitaxel monotherapy are observed with doses as low as 50 mg/kg/d[1].

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 : 125 mg/mL (195.36 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5629 mL 7.8146 mL 15.6292 mL
5 mM 0.3126 mL 1.5629 mL 3.1258 mL
10 mM 0.1563 mL 0.7815 mL 1.5629 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

FL5.12 cells suspended in EMB growth medium containing 4% fetal bovine serum (FBS) are incubated at 37°C for 1 hour in 10 μM A-385358. Compound concentration is determined by high-performance liquid chromatography before and after the 1-hour incubation following brief centrifugation. To analyze membrane-bound fractions following compound incubation, cells are washed once with 10 volumes of cold PBS and lysed with 4 mL of water. A-385358 concentration is determined from aliquots of lysate before and after centrifugation[1].

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

Cell Assay
[1]

A549 cells (1×105) are plated in 96-well plates in medium containing 10% fetal bovine serum. Following attachment, A-385358 is added to one set of wells (final concentration of 50 μM in 10% FBS) and medium is added to another set. [3H]Paclitaxel (5 μM; 0.5 μCi/mL final concentration) is added to all wells and the cells are incubated at 37°C for various periods of time. For washout experiments, cells are exposed first to [3H]paclitaxel for 2 hours. The cells are washed once with medium and then incubated with fresh medium with or without 50 μM A-385358 at 37°C for various periods of time[1].

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

Animal Administration
[1]

For efficacy studies, male CD-1 nude mice are inoculated with a 1:5 dilution of tumor brei in 50% Matrigel and analysis is conducted. A-385358 is delivered in a vehicle containing 5% Tween 80, 20% propylene glycol, and 75% PBS (pH 3.8). Paclitaxel is formulated according to the recommendations of the manufacturer. For combination therapy of paclitaxel plus A-385358, both drugs are administered i.p. with the paclitaxel given several hours before treatment with A-385358 (except for immunohistochemistry studies looking at expression of MPM-2 and caspase-3 wherein the two drugs are given simultaneously)[1].

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

References
Molecular Weight

639.83

Formula

C₃₂H₄₁N₅O₅S₂

CAS No.

406228-55-5

SMILES

O=C(NS(=O)(C1=CC=C(N[[email protected]@H](CSC2=CC=CC=C2)CCN(C)C)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCC(C)(C)CC4)C=C3

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
A-385358
Cat. No.:
HY-16014
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A-385358

Cat. No.: HY-16014