| 产品描述： | S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. 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. |
| 体外研究： |
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. |
| 体内研究： |
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. |
| 参考文献： |
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. |
| 保存条件： |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.226 ml |
6.132 ml |
12.265 ml |
| 5 mM |
0.245 ml |
1.226 ml |
2.453 ml |
| 10 mM |
0.123 ml |
0.613 ml |
1.226 ml |
| 50 mM |
0.025 ml |
0.123 ml |
0.245 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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