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抑制剂/激活剂

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凋亡与自噬

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S63845

S63845是一种新型的、选择性的MCL-1抑制剂，Kd值为0.19 nM。对其他Bcl-2成员，如Bcl-2或Bcl-xL，没有明显结合能力。

货号：
TK0158
规格：

1mg
价格：
￥0.00

产品参数

CAS No.	1799633-27-4
生物活性	S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.
分子式	C39H37ClF4N6O6S
分子量	829.26
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 33.33 mg/mL (40.19 mM; Need ultrasonic)
体内研究	S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.
体外研究	The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM).
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纯度及产品资料	98%

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