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编 号:F744983
分子式:C22H28N2O6S
分子量:448.53
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生物活性:
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 μM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity.

体内研究:
Antitumor agent-87 (0.1 μg/egg) 在鸡胚中表现出抗肿瘤活性。Animal Model:chick embryos (HT-1080CYP1A1, HT-1080empty, HT-1080 cells)
Dosage:0.1 μg/egg
Administration:
Result:Did not show statistically significant antitumor activity on grafted cell lines devoid of CYP1A1 (HT-1080 and HT-1080empty), showed antitumoral inhibition of 29% on the grafted HT-1080CYP1A1.

体外研究:
Antitumor agent-87 (compound 10) 在人肝微粒体、小鼠肝微粒体和大鼠肝微粒体中的半衰期 (t1/2) 分别为 70、44、107 分钟。Antitumor agent-87 (1250 nM) 诱导细胞周期停滞在 G2/M 期。Antitumor agent-87 (0-12500 nM; 72 h) 具有抗增殖活性,对 HT-1080CYP1A1, HT-1080empty, HT-1080, MDA-MB-231, MDA-MB-468, T47D, SK-BR-3, MCF7细胞的 IC50 值分别为 500, 8800, 6800, >12500, 210, 1100, 79, 43 nM。
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