半岛bd体育手机客户端 说明
一般描述
A cell-permeable, reversible and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as a kinase inhibitor for Src, eEF2-K, and PKA (IC50= 2.2, 3.2, and 9.6 ?M, respectively). Inhibits EGFR-K and PKC only at much higher concentrations (IC50= 320 ?M). Reported to exhibit potent anti-tumor activity (EC50= 3.66 and 39 ?M in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-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, reversible, and substrate-competitive arylidene-cyclopentenedione derived tyrphostin that acts as an inhibitor for Src, eEF2-K, and PKA (IC50= 2.2, 3.2, and 9.6 ?M, respectively), while it inhibits EGFR-K and PKC at much higher concentrations (IC50= 320 ?M). Displays potent antitumor activity (EC50= 3.66 and 39 ?M in HepG2 and HCT116 tumor cells, respectively) with greatly reduced mitochondrial- (≥1000-fold) and hepato-toxicity (≥50-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: 2.2, 3.2, and 9.6 ?M against Src, eEF2-K, and PKA, respectively
Primary Target
Src
Product competes with ATP.
Reversible: yes
警告
Toxicity: Harmful (C)
重悬
Following reconstitution, aliquot and freeze (- 20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Hori, H., et al. 2003.Cell. Mol. Biol. Lett.8,528.
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 | C20H24O3 |
分子量 | 312.40 |
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 | yellow |
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 |
Sigma-Aldrich