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EGFR Inhibitor II, BIBX1382-CAS 196612-93-8-Calbiochem

品牌
Sigma-Aldrich
CAS
196612-93-8
货号
324832
规格纯度
The EGFR Inhibitor II, BIBX1382, also referenced under CAS 196612-93-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
参考价格
3945.15 *本价格含增值税费
促销
数量
-+
产品介绍:

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/tradenameCalbiochem®
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
WGKWGK 2
闪点(F)Not applicable
闪点(C)Not applicable

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