供货周期: | 一周 |
品牌: | 爱必信 |
规格: | 98% |
货号: | abs821017 |
CAS号: | 1616420-30-4 |
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抑制剂描述: 产品名称:CFI-400945 fumarate 产品别名:见爱必信官网 英文别名:CFI-400945 fumarate 靶点:PLK CAS:1616420-30-4 纯度:98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder) 描述:CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively. 溶解性: 体外研究: CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC50s of 2.8, 6, 9, 140, 98, 22 nM, and EC50s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC50s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) . CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC50 value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death. 体内研究:CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC50s of 2.8, 6, 9, 140, 98, 22 nM, and EC50s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC50s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) . CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC50 value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death.
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