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编 号:F756923
分子式:C18H19N3O3
分子量:325.36
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生物活性:
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity.

体内研究:
Tubulin inhibitor 32 (50、100 mg/kg;口服;每日一次,持续 20 天) 在小鼠体内显示出抗肿瘤活性。Animal Model:4-6 weeks old male nude mice (HCT-116 tumor model)
Dosage:50, 100 mg/kg
Administration:P.o.; daily for 20 days
Result:Decreased the tumor volume and tumor weight by 44.1% and 27.0% at the dose of 50 mg/kg, respectively

体外研究:
Tubulin inhibitor 32 (compound 6y) (0-2 μM; 24 h) 以剂量依赖性方式抑制 HCT-116 细胞中集落的形成。Tubulin inhibitor 32 (0-100 μM; 24 h) 抑制微管聚合,IC50 值为 8.4 μM。Tubulin inhibitor 32 (0-2 μM; 24, 48 h) 诱导细胞凋亡和细胞周期停滞在 G2/M 期。Tubulin inhibitor 32 在人肝微粒体和大鼠肝微粒体中表现出代谢稳定性,T1/2 值分别为 106.2,6.9 min。
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