6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐
- CAS号:174634-09-4
- 英文名:TAS 103
- 中文名:6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐
- CBNumber:CB62668727
- 分子式:C20H21Cl2N3O2
- 分子量:406.30564
- MOL File:174634-09-4.mol
- 储存条件 :under inert gas (nitrogen or Argon) at 2-8°C
- 溶解度 :PBS (pH 7.2):1.0(Max Conc. mg/mL);2.46(Max Conc. mM)
- 形态 :A crystalline solid
- 颜色 :Brown to orange
6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐性质、用途与生产工艺
- 生物活性 TAS-103 dihydrochloride 是一种 DNA 拓扑异构酶 I/II (topoisomerase I/II) 双重抑制剂,可用于癌症研究。
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靶点
Topoisomerase I
Topoisomerase II
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体外研究
TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC 50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103. TAS-103 inhibits the viability of HeLa cells, with an IC 50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation.
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体内研究
TAS-103 (30 mg/kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103.
- 更新日期:2025/02/08
- 产品编号:HY-13758A
- 产品名称:6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐 TAS-103 dihydrochloride
- CAS编号:174634-09-4
- 包装:1 mg
- 价格:500元
- 更新日期:2025/02/08
- 产品编号:HY-13758A
- 产品名称:6-[[2-(二甲基氨基)乙基]氨基]-3-羟基-7H-茚并[2,1-C]喹啉-7-酮二盐酸盐 TAS-103 dihydrochloride
- CAS编号:174634-09-4
- 包装:5mg
- 价格:1100元
- 公司名称:A.J Chemicals
- 联系电话:--
- 电子邮件:sales@ajchem.in
- 国家:印度
- 产品数:6100
- 优势度:58