RGB-286147 是一种选择性和 ATP 竞争性CDK和 CDK 相关激酶 (CRK) 抑制剂，IC50值范围为 9-839 nM。RGB-286147 对其他非 CDK/CRK 激酶的活性较低。RGB-286147 诱导细胞凋亡 (apoptosis)，并具有抗肿瘤活性。
| 生物活性 | RGB-286147 is a selective and ATP-competitiveCDKandCDK-related kinases (CRK)inhibitor withIC50values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cellapoptosis, and exhibits anti-tumor activity[1]. |
| IC50& Target[1] | CDK1/cyclinB 48 nM (IC50) | CDK2/E 15 nM (IC50) | CDK4/D1 839 nM (IC50) | cdk6/cyclin D3 232 nM (IC50) |
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体外研究
(In Vitro) | RGB-286147 (50-100 nM; 24-48 hr) induces cell cycle arrest in the G1 phase, causes a marked inhibition of DNA replication, and induces apoptosis in HCT116 cells[1].
RGB-286147 (100 nM; 48 hr) results in proteolytic cleavage of PARP in HCT116 cells[1].
RGB-286147 (24-72 hr) shows potent and irreversible cell killing activity in HCT116 cells. The IC50value for inhibition of colony formation by RGB-286147 is 57 nM[1].
RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50value of<10 nm for 60 tumorigenic cell lines. and also inhibits growth of non-cycling hct116 cells with an ic50value of 40 nM[1].
Cell Cycle Analysis[1] | Cell Line: | HCT116 cells | | Concentration: | 50 nM and 100 nM | | Incubation Time: | 24 or 48 hr | | Result: | Caused a marked inhibition of DNA replication and induced cell cycle arrest. |
Western Blot Analysis[1] | Cell Line: | HCT116 cells | | Concentration: | 100 nM | | Incubation Time: | 48 hr | | Result: | Resulted in proteolytic cleavage of PARP. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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