CDK5 inhibitor 20-223

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CDK5 抑制剂 20-223 (CP 668863) 有效、选择性、ATP 竞争性 CDK2/5 抑制剂，对于 CDK2/CyclinE 和 CDK5/p35 的 IC50 分别为 6.0 和 8.8 nM，对 CDK1/4/6/7/ 几乎没有活性9.

CDK5 inhibitor 20-223 (CP 668863) potent, selective, ATP-competitive CDK2/5 inhibitor with IC50 of 6.0 and 8.8 nM for CDK2/CyclinE and CDK5/p35, with little to no activity against CDK1/4/6/7/9; decreases pRB (S807/811) and pFAK (S732) levels in CRC cell lines, effectively blocks the kinase activity of CDK2 and CDK5 in multiple CRC cell lines; reduces migration of CRC cells, reduces cell growth in a panel of human CRC cell lines with mean IC50 of 362 nM; effectively slows tumor progression in mice models.

Cell Viability Assay Cell 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 Analysis Cell 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).

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.

CP 668863

Angiogenesis

CDK

CDK

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865317-30-2

305.381

C19H19N3O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (327.47 mM)

——

N-(3-cyclobutyl-1H-pyrazol-5-yl)-2-(naphthalen-2-yl)acetamide

(-20℃)

With Ice Pack

≥ 2 years