865317-30-2
中文名稱
CDK5 INHIBITOR 20-223
英文名稱
CDK5 inhibitor 20-223
(CP 668863)
CAS
865317-30-2
分子式
C19H19N3O
分子量
305.37
MOL 文件
865317-30-2.mol
更新日期
2023/03/20 15:41:25
865317-30-2 結構式
基本信息
英文別名
CDK5 inhibitor 20-223CDK5 inhibitor 20-223 (CP 668863)
2-Naphthaleneacetamide, N-(5-cyclobutyl-1H-pyrazol-3-yl)-
所屬類別
生物化工：抑制劑常見問題列表
生物活性
CDK5 inhibitor 20-223 是一種有效的 CDK2 和 CDK5 抑制劑，IC50 分別為 6.0 和 8.8 nM。CDK5 inhibitor 20-223 有潛力用于結腸直腸癌 (CRC) 的研究。靶點
|
CDK2 6.0 nM (IC 50 ) |
CDK5 8.8 nM (IC 50 ) |
體外研究
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. |
體內研究
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. |