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CAS No.: 174634-09-4

TAS-103 2HCl Catalog No. CSN17261

Synonyms: BMS-247615 dihydrochloride;BMS-247615 2HCl;TAS 103 (hydrochloride)

TAS-103 2HCl is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

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400-920-2911

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技术信息

生物活性

描述Eukaryotic DNA topoisomerases I and II are essential nuclear enzymes responsible for the organization and modulation of the topological features of DNA and facilitate cell replication, transcription and repairment of genetic information. TAS-103 can inhibit both topoisomerase I and topoisomerase (topo) II, which stabilizes topo I, topo IIα, and topo IIβ cleavable complexes in purified enzyme cleavable complex assay， but shows a preference for topo IIα in whole cells using the TARDIS assay. TAS-103 at concentration ranging in 7nM-200nM for 24h induced an increase of cell population in the S-G2/M phase and strong cytotoxicity in S-phase cells. TAS-103 showed strong antitumor effect and broad-spectrum, growth-inhibitory effect (IC50 ranging in 3–230 nM), but showed much less potency to cells bearing a Topo I gene mutation, such as PC-7/CPT cells, and cells with decreased Topo II expression, such as KB/VM4 and HT-29/Etp cells.
动物研究
剂量
Mice: 30 mg/kg^[3] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[3] (i.v.)
给药途径	i.v.

[1] Ewesuedo RB, Iyer L, et al. Phase I clinical and pharmacogenetic study of weekly TAS-103 in patients with advanced cancer. J Clin Oncol.
[2] Parajuli P, Yano S, Nishioka Y, Nokihara H, Hanibuchi M, Nishimura N, Utsugi T, Sone S. Therapeutic efficacy of a new topoisomerase I and II inhibitor TAS-103, against both P-glycoprotein-expressing and -nonexpressing drug-resistant human small-cell lung cancer. Oncol Res. 1999;11(5):219-24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4612 mL
- 12.3060 mL
- 24.6120 mL
- 5 mM
- 0.4922 mL
- 2.4612 mL
- 4.9224 mL
- 10 mM
- 0.2461 mL
- 1.2306 mL
- 2.4612 mL

技术信息

CAS号

174634-09-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21Cl2N3O2

运输

蓝冰

分子量

406.31

别名

BMS-247615 dihydrochloride;BMS-247615 2HCl;TAS 103 (hydrochloride);TAS-103;TAS 103 HCl;BMS-247615 HCl,

溶解度

Water

50.0 mg/mL (123.1 mM) warming

动物实验配方

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