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TAS-103 dihydrochloride

TAS-103 dihydrochloride

产品编号 T7309   CAS 174634-09-4
别名: 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, TAS-103 (dihydrochloride), BMS-247615 dihydrochloride

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) 是可用于癌症研究的一种 DNA 拓扑异构酶 I/II 双重抑制剂。

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TAS-103 dihydrochloride Chemical Structure
TAS-103 dihydrochloride, CAS 174634-09-4
规格 价格/CNY 货期 数量
1 mg ¥ 398 现货
5 mg ¥ 898 现货
10 mg ¥ 1,360 现货
25 mg ¥ 2,890 现货
50 mg ¥ 4,320 现货
100 mg ¥ 6,170 现货
其他形式的 TAS-103 dihydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: TAS-103 dihydrochloride (T7309)
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参考文献
产品描述 TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II.
体外活性 The in vitro antitumor effects of TAS-103 were compared with those of other known Topo I and Topo II inhibitors. TAS-103 inhibited DNA synthesis more strongly than RNA and protein synthesis, and induced an increase of cell population in the S-G2/M phase. The cytotoxicity of TAS-103 was strongest against S-phase cells, but its cell cycle phase specificity was not clear, and depended on drug concentration and exposure time. The cytotoxicity of TAS-103 (IC50: 0.0030-0.23 microM) against various tumor cell lines was much stronger than that of VP-16 and comparable to that of SN-38. The cytotoxicity of TAS-103 seemed to be more related to the amount of protein-DNA complexes than to the accumulation of TAS-103 in the cells. P-Glycoprotein (P-gp)-mediated MDR, CDDP-resistant and 5-FU-resistant cell lines did not show cross-resistance to TAS-103. Although PC-7/CPT cells bearing a Topo I gene mutation showed cross-resistance to TAS-103, the sensitivity of P388/CPT, HT-29/CPT and St-4/CPT cells, showing decreased Topo I expression, was not changed. KB/VM4 and HT-29/Etp cells, showing decreased Topo II expression, were slightly cross-resistant to TAS-103. These results suggest that TAS-103 may act as an inhibitor of both Topo I and Topo II at the cellular level[1].
别名 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, TAS-103 (dihydrochloride), BMS-247615 dihydrochloride
分子量 406.31
分子式 C20H21Cl2N3O2
CAS No. 174634-09-4

存储

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

溶解度

H2O: 50 mg/mL (123.06 mM), Sonication is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.4612 mL 12.3059 mL 24.6117 mL 61.5294 mL
5 mM 0.4922 mL 2.4612 mL 4.9223 mL 12.3059 mL
10 mM 0.2461 mL 1.2306 mL 2.4612 mL 6.1529 mL
20 mM 0.1231 mL 0.6153 mL 1.2306 mL 3.0765 mL
50 mM 0.0492 mL 0.2461 mL 0.4922 mL 1.2306 mL
100 mM 0.0246 mL 0.1231 mL 0.2461 mL 0.6153 mL

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TargetMol Library Books参考文献

1. Aoyagi Y , Kobunai T , Utsugi T , et al. In vitro Antitumor Activity of TAS-103, a Novel Quinoline Derivative That Targets Topoisomerases I and II[J]. Japanese journal of cancer research: Gann, 1999, 90(5):578-587. 2. Ishida K , Asao T . Self-association and unique DNA binding properties of the anti-cancer agent TAS-103, a dual inhibitor of topoisomerases I and II[J]. Biochimica et Biophysica Acta, 2002, 1587(2-3):155-163.
Levofloxacin Epirubicin hydrochloride Guajadial C SN-38 Coralyne chloride Rebeccamycin Doxorubicin hydrochloride Ofloxacin

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗癌活性化合物库 已知活性化合物库 经典已知活性库 NO PAINS 化合物库 抗癌化合物库 ReFRAME 相关化合物库 抗衰老化合物库 DNA 损伤和修复分子库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TAS-103 dihydrochloride 174634-09-4 DNA Damage/DNA Repair Topoisomerase TAS-103 TAS 103 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 inhibit TAS 103 dihydrochloride TAS-103 Dihydrochloride TAS-103 (dihydrochloride) Inhibitor TAS103 dihydrochloride BMS-247615 Dihydrochloride TAS103 Dihydrochloride TAS103 BMS-247615 BMS 247615 BMS-247615 dihydrochloride BMS 247615 Dihydrochloride TAS 103 Dihydrochloride BMS247615 BMS247615 Dihydrochloride inhibitor

 

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