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A-385358

CAS No. : 406228-55-5

MCE 站：A-385358

产品活性：A-385358 是 Bcl-X_L 的一个选择性抑制剂，对于 Bcl-X_L 和 Bcl-2 的 K_i 值分别为 0.80 和 67 nM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vitro: A-385358 is a selective inhibitor of Bcl-X_L with K_is of 0.80 and 67 nM for Bcl-X_L and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-X_L 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-X_L 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-X_L cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-X_L versus Bcl-2 cells.

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.

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