A-385358 is a selective inhibitor of Bcl-X L with K i s of 0.80 and 67 nM for Bcl-X L and Bcl-2 , respectively. In Vitro A-385358 is a selective inhibitor of Bcl-X L with K i s 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 EC 50 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 EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 mm 3 (%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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Bcl-xL 0.8 nM (Ki) Bcl-2 67 nM (Ki)
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A-385358
CAS number：406228-55-5 molecular formula：C32H41N5O5S2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 406228-55-5 | molecular formula | C32H41N5O5S2 |
| molecular weight | 639.83 g/mol | Exact mass | ≥98% |
| PSA | 161.000 Ų | logp | 7.200 |
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