| 应用 |
A Plk inhibitor with efficacy against 32 cancer cell lines. |
| 产品介绍 |
BI 2536是一种有效的Plk1抑制剂，IC50为0.83 nM，比作用于Plk2和Plk3选择性分别高4和11倍。 |
| 备注 |
BI2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. Phase 2. |
| 生化机理 |
BI 2536 treatment ranging from 10 nM to 100 nM blocks the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibits of cohesin release from chromosome arms, and induces monopolar spindle formation and other Plk1 dependent processes. BI 2536 treatment leads to the HeLa cells arrested in the G2/M stage. BI 2536 inhibits the growth of a panel of 32 human cancer cell lines with EC50 of 2-25 nM. |
| 别名 |
4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺;BI-2536; BI2536;BI-2536; BI2536;4-[[(7R)-8-Cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)benzamide; Boehringer PLK-1 inhibitor |
