| 生化机理 |
Description:
IC50 Value: 3 nM (PLK1) [1]
RO3280 exhibits potent antiproliferative activity in a wide range of cancer cell lines, and shows strong anti-tumor activities in an in vivo HT-29 colorectal xenograft mouse model.
Difluoro-analog 7 (RO3280) gave the best results in both enzymatic (PLK1, IC50 = 3 nM) and cellular (lung cancer cell line H82, EC50 = 6 nM) assays. RO3280 was evaluated for its in vivo antitumor activity in a series of mouse xenograft models, of which the HT-29 colorectal cancer cell line is representative. RO3280 displayed robust antitumor activity ranging from 72% tumor growth inhibition when dosed once weekly at 40 mg/Kg, to complete tumor regression when dosed more frequently.
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| 别名 |
Ro5203280;Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-;Ro5203280;Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-N-(1-methyl-4-piperidinyl)- |
