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编 号:F041301
分子式:C17H15N5S
分子量:321.4
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生物活性:
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines.

体内研究:
AG311 (23 mM; intratumoral; once daily for 2 days) 在小鼠中增加癌细胞坏死。AG311 (45 mg/kg; i.p.; twice weekly for 30 days) 抑制小鼠肿瘤生长和肺转移。Animal Model:BALB/cJ mice, 4T1 Triple Negative Orthotopic Allograft
Dosage:23 mM, 1/15 of tumor volume
Administration:Intratumoral injection, once daily for 2 days
Result:Injected tumors had a significantly higher percentage of necrosis compared with their control-treated counterparts.
Animal Model:7-week-old female NCr nu/nu athymic mice, MDA-MB-435 Orthotopic Xenograft
Dosage:45 mg/kg
Administration:Intraperitoneal injection, twice weekly for 30 days
Result:Significantly reduced primary tumor growth. Animals had fewer lung metastases at the end of the experiment compared with control-treated animals.

体外研究:
AG311 (0-30 μM; 48 h) 显示对癌细胞的细胞毒性。AG311 (10-40 μM; 0-150 min) 选择性诱导乳腺癌细胞膜透性 (与 HUVECs 相比)。Ag311 (25 μm;20 min)诱导MDA-MB-435细胞坏死,缺乏凋亡分子标志物。AG311 (25 μM; 20 min) 影响 MDA-MB-435 细胞钙稳态和质膜去极化。AG311 (5-20 μM) 诱导 MDA-MB-435 细胞线粒体膜快速改变和线粒体功能障碍。AG311 (0-14 μM; 30 h) 抑制乳腺癌细胞迁移。
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