324842
EGFR/ErbB-2/ErbB-4 Inhibitor II - CAS 944341-54-2 - Calbiochem
The EGFR/ErbB-2/ErbB-4 Inhibitor II, also referenced under CAS 944341-54-2, controls the biological activity of EGFR/ErbB-2/ErbB-4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
EGFR/ErbB-2/ErbB-4 Inhibitor II - CAS 944341-54-2 - Calbiochem, (E)-4-Amino-6-(4-benzyloxy-3-chloro-phenylamino)-pyrimidine-5-carbaldehyde-O-(2-morpholin-4-yl-ethyl)-oxime, HCl, JNJ-28871063, HCl
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About This Item
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质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
beige
溶解性
DMSO: 25 mg/mL
运输
ambient
储存温度
−20°C
一般描述
A cell-permeable aminopyrimidine oxime compound that potently inhibits EGFR/ErbB1/HER1, ErbB2/HER2/neu, and ErbB4/HER4 kinase activity (IC50 = 22, 38 and 21 nM, respectively) in an ATP-competitive manner and effectively suppresses cellular receptor phosphorylation (IC50 = 223 and 107 nM against basal HER2 and EGF-induced EFGR phosphorylation, respectively, in SKBR3 and A431 cultures) as well as HER2- and EGFR-dependent cancer cell proliferations (IC50<1µM), while exhibiting much reduced or little activity against a panel of 202 other kniases. Reported to be orally available and blood-brain barrier permeant in both mice and rats and be efficacious in inhibiting tumor growth in several murine xenograft models (100 to 200 mg/kg/day, p.o.) in vivo.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
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
Emanuel, S.L., et al. 2008. Mol. Pharmacol.73, 338.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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