产品
编 号:F757098
分子式:C25H20N4O2
分子量:408.45
产品类型
结构图
CAS No: 2948304-00-3
联系客服
产品详情
生物活性:
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research.
体内研究:
AMPK activator 11 (Compound 18a) (2.5 或 10 mg/kg 腹腔注射,持续 25 天) 选择性抑制 RKO 细胞体外异种肿瘤模型的肿瘤生长,且无毒性>。Animal Model:RKO cells related axenograft model on male BALB/nude mice
Dosage:2.5 or 10 mg/kg
Administration:Intraperitoneal injection (i.p.) for 25 days
Result:Resulted in 58.2% tumor growth inhibition, with no significant weight loss observed.Resulted in 77.1% inhibition of tumor growth but also caused a 36% weight loss. Immunohistochemistry results also showed activation of AMPK in tumor tissue.
体外研究:
AMPK activator 11 (Compound 18a) (0-30 μM;0-7 天) 抑制 CRC 细胞的生长和迁移,对其 IC50 值低于 1 μM。AMPK activator 11 (0-0.1 μM;24 小时) 显著提高 RKO 细胞的全局耗氧率 (OCR) ,同时细胞外酸化率 (ECAR) 轻微变化。AMPK activator 11 上调 p-AMPK 和线粒体复合物 III 和 V 的表达,并且具有在 CRC 中选择性激活 OXPHOS 的能力。