CDK5 inhibitor 20-223 (C09-1121-130)

CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC 50 s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agentIn VitroCDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines. ?/nCDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells Concentration: 10 μM, 1 μM, 100 nM, 10 nM Incubation Time: 72 hours Result: Reduced cell growth. IC50s of 168±20, 480±41, 360±72, 763±92, 117±49, 568±49, 79±31 nM for SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells. Western Blot AnalysisCell Line: CRC cell lines GEO, HCT116 and HT29 Concentration: 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM Incubation Time: 6 hours Result: Did not affect the total levels of CDK2/5, and the levels of total FAK or total Retinoblastoma protein (Rb). Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.In VivoCDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic nude mice Dosage: 8 mg/kg Administration: Injections were given subcutaneously daily for the first week and every other day for two more weeks for a total of 14 injections. Result: Reduced tumor growth and tumor weight in vivo.IC50& Target:CDK2 6.0 nM (IC 50 ) CDK5 8.8 nM (IC 50 ). Specification: 10mM in DMSO Molecular Formula: C19H19N3O Molecular Weight: 305.37