BMS-599626 2HCL(714971-09-2 Free base)
作者：齐岳
发布时间：2023-08-25
08:58:38
点击数：
产品名称：BMS-599626 2HCL(714971-09-2 Free base)
产品描述：
| 产品描述 | BMS-599626 2HCL is a BMS-599626 derivative.BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively.BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy. |
| 靶点活性 | HER1 inhibitor:20 nM, HER4:190 nM, HER2 inhibitor:30 nM |
| 体外活性 | BMS-599626 is a potent HER inhibitor and has a higher inhibition ability than the other reported inhibitors. When tested with breast tumor cell lines (HCC202, HCC1942 and AU565) that highly expressed HER1 and HER2, BMS-599626 treatment inhibited cell proliferation, while having no effect on A2780 cells without HER1 or HER2 expression.[1]Treated OV202 cells with BMS-599626 significantly inhibited cell proliferation and enhanced cell apoptosis by inhibiting HER.[3]When tested with Sal2 cells expressing CD8-HER2 fusion protein, BMS-599626 treatment inhibited the receptor phosphorylation and MAPK phosphorylation with the IC50 value of 0.3 and 0.22 μM/L, respectively.[1] |
| 体内活性 | In mouse models with Sal2 tumor cells xenograft, oral administration of BMS-599626 inhibited Sal2 cells growth in a dose-dependent manner and significantly delayed tumor growth at the concentration of 60 mg/kg.[1] |
| 别名 | AC480 2HCl, BMS-599626 2HCL(714971-09-2 Free base) |
| 分子量 | 603.47 |
| 分子式 | C27H29Cl2FN8O3 |
| CAS No. | 1781932-33-9 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 25 mg/mL (41.43 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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