TRi-1

99.20%

TRi-1

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品牌：源叶(MedMol)

产品编号：S87818 一键复制产品信息

CAS号：246020-68-8

分子式：C₁₂H₉ClN₂O₅S

分子量：328.73

货号	规格	价格	上海	北京	珠海	重庆	武汉
S87818-2mg	99.20%	￥720.00 S87818-2mg ￥720.00 现货	2 2	-	-	-	-
S87818-5mg	99.20%	￥1080.00 S87818-5mg ￥1080.00 现货	5 5	-	-	-	-
S87818-10mg	99.20%	￥1720.00 S87818-10mg ￥1720.00 现货	1 1	-	-	-	-
S87818-25mg	99.20%	￥3110.00 S87818-25mg ￥3110.00 现货	1 1	-	-	-	-
S87818-50mg	≥98%	￥4200.00 S87818-50mg ￥4200.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献(4篇) 质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

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

靶点：

IC50: 12 nM (TXNRD1)

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。 Western Blot Analysis Cell Line: FaDu cells Concentration: 0.679 and 6.79 μM Incubation Time: 6 h Result: Efficiently activated JNK and p38 phosphorylation. Cell Cytotoxicity Assay Cell Line: Leukemia, non-small cell lung, CNS, colon, melanoma, ovarian, renal, prostate and breast cancer cells Concentration: 10 nM-100 μM Incubation Time: 48 h Result: Displayed potency against every cell line tested, with an average growth inhibition to 50% (GI50) of 6.31 μM.

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.

参考文献：

1. Stafford WC, et al. Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy. Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444.

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.042 ml	15.21 ml	30.42 ml
5 mM	0.608 ml	3.042 ml	6.084 ml
10 mM	0.304 ml	1.521 ml	3.042 ml
50 mM	0.061 ml	0.304 ml	0.608 ml