| Bioactivity | FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc-), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model[1]. |
| Invitro | FA16 (1 μM; 5 min) 在大鼠和人肝微粒体中具有满意的代谢稳定性[1]。FA16 (5 μM; 10 h) 诱导 HT1080 细胞中脂质 ROS 积累并抑制谷氨酸释放[1]。FA16 (5 μM; 24 h) 结果线粒体萎缩，膜密度增大，符合铁衰相关的形态特征[1]。FA16 (10 μM; 24 h) 诱导的铁死亡能够被铁脱落抑制剂 Fer-1、Trolox 或 DFO 挽救，而凋亡或坏死抑制剂则对其无效[1]。Parameter |
| In Vivo | FA16 (15 或 30 mg/kg; 腹腔注射; 隔天给药, 共 21 天) 在 786-O 异种移植物小鼠模型中显著抑制肿瘤生长，安全性好 (不引起体重下降)，还诱导肿瘤组织中发生铁死亡[1]。 Animal Model: |
| Name | FA16 |
| Formula | C22H25F3N4O2S |
| Molar Mass | 466.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fang Y, et al. Discovery and optimization of 2-(trifluoromethyl)benzimidazole derivatives as novel ferroptosis inducers in vitro and in vivo. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114905. |