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1174664-88-0

中文名稱 VER-158411
英文名稱 VER-158411
CAS 1174664-88-0
分子式 C31 H34 N6 O3
MOL 文件 1174664-88-0.mol
1174664-88-0 結(jié)構(gòu)式 1174664-88-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T17223
英文別名
V-158411
VER-158411
174664-88-0
VER-00158411
1H-Pyrazole-4-carboxamide, N-[5-[5-[3-(dimethylamino)-2,2-dimethylpropoxy]-1H-indol-2-yl]-1,6-dihydro-6-oxo-3-pyridinyl]-1-(phenylmethyl)-

應(yīng)用領(lǐng)域

用途一
V158411 is a novel potent and selective Chk1 inhibitor. Inhibition of Chk1 with the small molecule inhibitor V158411 induces DNA damage and cell death in an unperturbed S-phase. V158411 abrogated gemcitabine and camptothecin induced cell cycle checkpoints, resulting in the expected modulation of cell cycle proteins and increased cell death in cancer cells. V158411 potentiated the cytotoxicity of gemcitabine, cisplatin, SN38 and camptothecin in a variety of p53 deficient human tumor cell lines in vitro, p53 proficient cells were unaffected. In nude mice, V158411 showed minimal toxicity as a single agent and in combination with irinotecan. In tumor bearing animals, V158411 was detected at high levels in the tumor with a long elimination half-life; no pharmacologically significant in vivo drug-drug interactions with irinotecan were identified through analysis of the pharmacokinetic profiles. V158411 potentiated the anti-tumor activity of irinotecan in a variety of human colon tumor xenograft models without additional systemic toxicity.
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