A-385358|406228-55-5|-陌孚医药/Medlife

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A-385358

目录号: PL04579 纯度: ≥98%

CAS No. :406228-55-5

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中文名称	A-385358
英文名称	A-385358
英文别名	N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-(4,4-dimethylpiperidin-1-yl)benzamide;Phenylpiperidine, 1a;BDBM21400;BCP18411;A17064;A 385358;N-[(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzene)sulfonyl]-4-(4,4-dimethylpiperidin-1-yl)benzamide;A-385358
Cas No.	406228-55-5
分子式	C₃₂H₄₁N₅O₅S₂
分子量	639.83
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	Bcl-xL 0.8 nM (Ki) Bcl-2 67 nM (Ki)
体外研究(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. has not ind
体内研究(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 (%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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Shoemaker AR, et al. A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res. 2006 Sep 1;66(17):8731-9.

溶解度数据	In Vitro: DMSO : 50 mg/mL (78.15 mM; Need ultrasonic)配制储备液

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