TX-1918-CAS 503473-32-3-Calbiochem

半岛bd体育手机客户端 说明

一般描述

A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC₅₀= 440 nM). Inhibits other kinases at much higher concentrations (IC₅₀= 4.4, 44, 44, and 440 ?M for Src, PKA, PKC, and EGFR-K, respectively). Reported to exhibit potent anti-tumor activity (EC₅₀= 2.07 and 230 ?M in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). May be useful as a therapeutic agent for cancer treatment in animal models.
A cell-permeable arylidene-cyclopentenedione derived tyrphostin that acts as a potent inhibitor for eEF2-K (IC₅₀= 440 nM), while it inhibits other kinases at much higher concentrations (IC₅₀= 4.4, 44, 44, and 440 ?M for Src, PKA, PKC, and EGFR-K, respectively). Displays potent antitumor activity (EC₅₀= 2.07 and 230 ?M in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥5000-fold) and hepato-toxicity (≥90-fold) when compared with another tyrphostin, AG 17 (Cat. No. 658425). It is therefore a more promising candidate as a therapeutic agent for cancer treatment.

包装

10 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Target IC₅₀: 440 nM against eEF2-K
Product does not compete with ATP.
Reversible: no
Primary Target
eEF2-K

警告

Toxicity: Harmful (C)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

其他说明

Hori, H., et al. 2002.Bioorg. Med. Chem.10,3257.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式	C14H12O3
分子量	228.24

半岛bd体育手机客户端 性质

质量水平	100
测定	≥95% (HPLC)
形式	solid
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze protect from light
颜色	light orange
溶解性	DMSO: 10 mg/mL
运输	ambient
储存温度	2-8℃

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 1
闪点(F)	Not applicable
闪点(C)	Not applicable