Name | CDK5 inhibitor 20-223 |
Synonyms | CDK5 inhibitor 20-223 CDK5 inhibitor 20-223(CP 668863) 2-Naphthaleneacetamide, N-(5-cyclobutyl-1H-pyrazol-3-yl)- |
CAS | 865317-30-2 |
Molecular Formula | C19H19N3O |
Molar Mass | 305.37 |
Appearance | Solid |
Storage Condition | 2-8°C,密封,干燥 |
biological activity | CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50 of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 has potential for research in colorectal cancer (CRC). |
Cell Line: | CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells CRC cell lines GEO, HCT116 and HT29 |
Concentration: | 10 μM, 1 μM, 100 nM, 10 nM 20, 10, 5, 2.5, 1.25, 0.625, 0.3125 μM |
Incubation Time: | 72 hours 6 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. 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. Reduced tumor growth and tumor weight in vivo. |
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. |