化合物FA16 T64357

Product Introduction
Bioactivity


英文名: FA16

描述: FA16 是一种选择性、代谢稳定的铁死亡 (ferroptosis) 诱导剂 ，IC50 值为1.26 μM。FA16 是 2-(三氟甲基) 苯并咪唑的衍生物。FA16 对胱氨酸/谷氨酸反转运蛋白 (system Xc-) 介导了细胞内谷氨酸和细胞外胱氨酸的交换有抑制作用。FA16 在 HepG2 异种移植瘤模型中显著抑制肿瘤生长。

体外活性: FA16 (1 μM; 5 min) has satisfactory metabolic stability in rat and human liver microsomes.[1]FA16 (5 μM; 10 h) induces lipid ROS accumulation and inhibits glutamate release in HT1080 cells.[1]FA16 (5 μM; 24 h) resulted in mitochondrial atrophy and increased membrane density, consistent with morphological characteristics related to iron failure.[1]Ferroptosis induced by FA16 (10 μM; 24 h) can be rescued by the iron-shedding inhibitors Fer-1, Trolox, or DFO, whereas apoptosis or necrosis inhibitors are ineffective.[1]

体内活性: FA16 (15 or 30 mg/kg; intraperitoneal injection; administered every other day for 21 days; BALB/c nude mice bearing HepG2 tumors (s.c.)) significantly inhibited tumor growth in the 786-O xenograft mouse model with TGI value of 47.6% and 77.1% at 15 and 30 mg/kg, respectively. FA16 was safe (did not cause weight loss), and also induced Ferroptosis occurs in tumor tissue.[1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.69 mg/mL (10 mM)


关键字: FA16

相关产品: Atorvastatin hemicalcium salt | (E)-Ferulic acid | Eugenol | Coenzyme Q10 | Piperazine Erastin | Sorafenib tosylate | SRS16-86 | Piperlongumine | SRS11-92 | Lepadin H

相关库: Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途