S65487 (VOB560) sulfate 是一种有效的选择性 Bcl-2 抑制剂。 S65487 sulfate 对 BCL-2 突变也有活性，例如 G101V 和 D103Y。S65487 sulfate 对 MCL-1，BFL-1 和 BCL-XL 的亲和力较差。S65487 sulfate 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。
货号:ajcx35864
CAS:2416937-01-2
分子式:C41H43ClN6O8S
分子量：815.33
溶解度:DMSO : 135 mg/mL (165.58 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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

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

S65487 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 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.