CDK5inhibitor20-223是一种有效的CDK2和CDK5抑制剂，IC50分别为6.0和8.8nM。CDK5inhibitor20-223有潜力用于结肠直肠癌(CRC)的研究。
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].
CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines[1].CDK5 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[1]. Cell Viability Assay[1] Cell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells
CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice[1]. Animal Model: Athymic nude mice[1]
[1]. Caroline M Robb, et al. Characterization of CDK(5) Inhibitor, 20-223 (Aka CP668863) for Colorectal Cancer Therapy. Oncotarget. 2017 Dec 28;9(4):5216-5232.
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