324840
EGFR/ErbB-2/ErbB-4 Inhibitor - CAS 881001-19-0 - Calbiochem
The EGFR/ErbB-2/ErbB-4 Inhibitor, also referenced under CAS 881001-19-0, 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 - CAS 881001-19-0 - Calbiochem, N-(4-((3-Chloro-4-fluorophenyl)amino)pyrido[3,4-d]pyrimidin-6-yl)2-butynamide
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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
protect from light
颜色
yellow
溶解性
DMSO: 4 mg/mL (Use fresh DMSO only.)
运输
ambient
储存温度
−20°C
一般描述
A cell-permeable, ATP-binding site-targeting alkynamidopyrimidine compound that acts as a potent and irreversible inhibitor of erbB activities (IC50 = 0.3, 1.1, and 0.5 nM for erbB-1, erbB-2, and erbB-4, respectively). Inhibits EGF- and heregulin-induced erbB autophosphorylation in NIH3T3-erbB-1 and in MDA-MB-453 cells (IC50 = 2.5 and 24 nM, respectively).
生化/生理作用
Cell permeable: yes
Primary Target
EGFR/ErbB-2/ErbB-4
EGFR/ErbB-2/ErbB-4
Product does not compete with ATP.
Reversible: no
Target IC50: 0.3, 1.1, and 0.5 nM for erbB-1, erbB-2, and erbB-4, respectively; 2.5 and 24 nM against EGF- and heregulin-induced erbB autophosphorylation in NIH3T3-erbB-1 and in MDA-MB-453 cells, respectively
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
Klutchko, S.R., et al. 2006. J. Med. Chem.49, 1475.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
10-13 - German Storage Class 10 to 13
Sylvester R Klutchko et al.
Journal of medicinal chemistry, 49(4), 1475-1485 (2006-02-17)
Structure-activity relationships for inhibition of erbB1, erbB2, and erbB4 were determined for a series of alkynamide analogues of quinazoline- and pyrido[3,4-d]pyrimidine-based compounds. The compounds were prepared by coupling the appropriate 6-aminoquinazolines or 6-aminopyrido[3,4-d]pyrimidines with alkynoic acids, using EDCI.HCl in pyridine.
Marie-Krystel Gauthier et al.
The European journal of neuroscience, 38(5), 2693-2715 (2013-06-14)
Spinal cord injury (SCI) results in degeneration of oligodendrocytes that leads to demyelination and axonal dysfunction. Replacement of oligodendrocytes is impaired after SCI, owing to the improper endogenous differentiation and maturation of myelinating oligodendrocytes. Here, we report that SCI-induced dysregulation
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