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编 号:F290794
分子式:C12H9ClN2O5S
分子量:328.73
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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生物活性:
TRi-1 is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1), with an IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.

体内研究:
TRi-1 (10 mg/kg;静脉注射;每天两次,持续 4 天或 5 mg/kg;腹腔注射;每周两次,持续 3 周) 损害人肿瘤异种移植物和同源小鼠肿瘤的生长和活力。Animal Model:SCID mice bearing established human FaDu cell xenografts
Dosage:10 mg/kg
Administration:Intravenous injection, twice a day for 4 days
Result:Resulted in decreased tumor growth compared to vehicle controls within four days with no signs of overt toxicity or changes in mouse weight relative to vehicle control.
Animal Model:PyMT-MMTV mice that spontaneously develop malignant breast cancer tumors
Dosage:5 mg/kg
Administration:Intraperitoneal injection, twice a week for 3 weeks
Result:Impaired tumor growth, significantly reduced tumor volumes.

体外研究:
TRi-1 (0.679 和 6.79 μM;6 小时) 对 FaDu 细胞中的细胞谷胱甘肽 (GSH) 浓度没有影响,有效激活 JNK 和 p38 磷酸化。 TRi-1 (2 μM) 以 NADPH 依赖性方式不可逆地抑制 TXNRD1。 TRi-1 (0.1-10 μM;0-10 h) 以浓度和时间依赖性方式在培养的 FaDu 细胞中增加 H2O2 产生。 TRi-1 (10 nM-100 μM;48 h) 显示出对癌细胞的细胞毒性。
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