CDK5 INHIBITOR 20-223

生物活性靶点体外研究体内研究 CDK5 INHIBITOR 20-223 试剂级价格

CAS号:865317-30-2
英文名:CDK5 inhibitor 20-223 (CP 668863)
中文名:CDK5 INHIBITOR 20-223
CBNumber:CB04844633
分子式:C19H19N3O
分子量:305.37
MOL File:865317-30-2.mol

CDK5 INHIBITOR 20-223化学性质

储存条件 :Store at -20°C
形态 :Solid
颜色 :Light yellow to yellow

CDK5 INHIBITOR 20-223性质、用途与生产工艺

生物活性 CDK5 inhibitor 20-223 是一种有效的 CDK2 和 CDK5 抑制剂，IC50 分别为 6.0 和 8.8 nM。CDK5 inhibitor 20-223 有潜力用于结肠直肠癌 (CRC) 的研究。
靶点

CDK2

6.0 nM (IC ₅₀ )

CDK5

8.8 nM (IC ₅₀ )

体外研究

CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines.
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.

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). Induced a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels.

体内研究

CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice.

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.