A-385358 是一种特异性 BCL-xL 抑制剂，对 BCL-xL 和 BCL-2 的 Ki 分别为 0.80 nM 和 67 nM。

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

In IL-3-deprived FL5.12/Bcl-XL cells, A-385358 results in cell killing with an EC50 of 0.47 μM and increases caspase-3 activity. The EC50 of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells with an EC50 of 1.9 μM which is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-XL cells. A-385358 stimulates more cytochrome c release from mitochondria isolated from FL5.12/Bcl-XL versus Bcl-2 cells[1].

The combination of A-385358 (75 mg/kg) plus paclitaxel (30 mg/kg) is well tolerated and inhibits tumor growth rate by nearly 80%. A-385358 exhibits slow but steady increase in the tumor growth. The combination of A-385358 (100 mg/kg) and a lower dose of paclitaxel produces a significant reduction in tumor growth and yields a >100% increase in time for tumors to reach 900 mm3 (%ILS)[1].

406228-55-5

C32H41N5O5S2

639.83

DMSO:125 mg/mL (195.36 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years