产品说明
一般描述
A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (10 mg/kg, daily, p.o.).
A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg).
包装
5 mg in Plastic ampoule
生化/生理作用
Cell permeable: yes
Target IC50: 3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells
Primary Target
EGFR (ErbB-1, HER-1)
Product competes with ATP.
Reversible: yes
警告
Toxicity: Irritant (B)
其他说明
Solca, F.F., et al. 2004. J. Pharm. Exp. Ther.311, 502.
Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun.281, 25.
Nuijen, B., et al. 2000. Int. J. Pharm.194, 261.
Tocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months.
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 | C18H19ClFN7 · 2HCl · 2H2O |
分子量 | 496.79 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | yellow |
溶解性 | water: 1 mg/mL DMSO: 25 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 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |