| 产品描述: | S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. 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. |
| 体外研究: |
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]. |
| 体内研究: |
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. |
| 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: |
2-8°C, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.327 ml |
6.634 ml |
13.268 ml |
| 5 mM |
0.265 ml |
1.327 ml |
2.654 ml |
| 10 mM |
0.133 ml |
0.663 ml |
1.327 ml |
| 50 mM |
0.027 ml |
0.133 ml |
0.265 ml |
|
| 注意: |
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