化合物TRi-1 T5481

Product Introduction
Bioactivity


英文名: TRi-1

描述: TRi-1 是不可逆的胞质硫氧还蛋白还原酶1 的特异性抑制剂(IC50:12 nM)。它有抗肿瘤作用，且线粒体毒性很小。

动物实验: Fox Chase male SCID mice were treated once with TRi-1 (0.7 to 10 mg/kg) or TRi-2 (0.5 to 20 mg/kg) via intravenous injections, and mouse health status was observed for up to 72 hours. For repeateddose toxicity studies with tumor-bearing animals, mice were first inoculated with 1*10^6 FaDu cells in phosphate-buffered saline at a preshaved region located at the anterior lateral thoracic wall . After 13 days of growth, tumors were measured by calipers, and treatments were initiated. Mice were injected with TRi-1 (10 mg/kg), TRi-2 (15 mg/kg), auranofin (10 mg/kg), or vehicle a total of nine times during a 5-day span via intravenous tail injection. Upon the final day of dosing, injections were performed subcutaneously due to hematomas in several of the mice at the tail injection site. Mouse health status was monitored daily, weight was measured, and tumor volume was recorded from caliper measurements.

体外活性: TRi-1在抑制人类肿瘤异种移植和同源小鼠肿瘤的生长及存活方面表现出显著效果，同时对线粒体毒性较小，且比auranofin具有更好的耐受性。

体内活性: TRi-1在小鼠肿瘤模型中的抗癌效力，与TXNRD1对于体内癌细胞生长的重要性这一观点相一致。

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

溶解度: DMSO : 62.5 mg/mL (190.13 mM)


关键字: antitumor | inhibit | TRi 1 | Inhibitor | TRi-1 | FaDu | thioredoxin reductase 1 | glutathione | TRi1 | TXNRD1

相关库: Mitochondria-Targeted Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Covalent Inhibitor 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