| Bioactivity | RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1]. |
| Invitro | 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 IC50 value for inhibition of colony formation by RGB-286147 is 57 nM[1]. RGB-286147 (48 hr) exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. And also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM[1]. Cell Cycle Analysis[1] Cell Line: |
| Name | RGB-286147 |
| CAS | 784211-09-2 |
| Formula | C23H22Cl2N4O3 |
| Molar Mass | 473.35 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |