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.
Synonym(s):
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
Empirical Formula (Hill Notation):
C17H11ClFN5O · 2.5H2O
CAS Number:
Molecular Weight:
400.79
UNSPSC Code:
12352200
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 4 mg/mL (Use fresh DMSO only.)
shipped in
ambient
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
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
Disclaimer
Toxicity: Standard Handling (A)
General description
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).
Other Notes
Klutchko, S.R., et al. 2006. J. Med. Chem.49, 1475.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
10-13 - German Storage Class 10 to 13
Certificates of Analysis (COA)
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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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