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Sigma-Aldrich

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(e):

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

Empirische Formel (Hill-System):
C17H11ClFN5O · 2.5H2O
CAS-Nummer:
881001-19-0
Molekulargewicht:
400.79
UNSPSC-Code:
12352200

Qualitätsniveau

100

Assay

≥95% (HPLC)

Form

solid

Hersteller/Markenname

Calbiochem®

Lagerbedingungen

OK to freeze
protect from light

Farbe

yellow

Löslichkeit

DMSO: 4 mg/mL (Use fresh DMSO only.)

Versandbedingung

ambient

Lagertemp.

−20°C

Allgemeine Beschreibung

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).

Biochem./physiol. Wirkung

Cell permeable: yes
Primary Target
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

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Klutchko, S.R., et al. 2006. J. Med. Chem.49, 1475.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Lagerklassenschlüssel

10-13 - German Storage Class 10 to 13

Analysenzertifikate (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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