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S65487 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
S65487 hydrochloride图片
CAS NO:1644543-95-2
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S65487 (VOB560) hydrochloride是一种有效的选择性 Bcl-2 抑制剂。S65487 hydrochloride 对 BCL-2 突变也有活性,例如 G101V 和 D103Y。S65487 hydrochloride 对 MCL-1,BFL-1 和 BCL-XL 的亲和力较差。S65487 hydrochloride 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。
Cas No.1644543-95-2
别名VOB560 hydrochloride
分子式C41H42Cl2N6O4
分子量753.72
溶解度DMSO : 90 mg/mL (119.41 mM; Need ultrasonic)
储存条件4°C, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

S65487 (VOB560) hydrochloride is a potent and selective Bcl-2 inhibitor. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities[1][2].

S65487 hydrochloride binds to the BH3 hydrophobic groove of BCL-2. S65487 hydrochloride induces apoptosis in a panel of hematological cancer cell lines and inhibits cell proliferation with IC50s in the low nM range[1].

S65487 hydrochloride induces complete regression in BCL-2-dependent RS4;11 tumors in vivo after a single IV (intravenous) administration. Strong and persistent tumor regression in xenograft models of lymphoid malignancies in mouse and rat are observed at well tolerated doses following weekly IV administration of S65487 hydrochloride in combination with the MCL-1-specific inhibitor, S64315/MIK665[1].

[1]. Arnaud Le Tiran, et al. Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax. Cancer Research. July 2021.

 
 
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