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
• Empirical Formula (Hill Notation): C₁₇H₁₁ClFN₅O · 2.5H₂O
• CAS Number: 881001-19-0
• Molecular Weight: 400.79
• UNSPSC Code: 12352200

Properties

• Quality Segment: 100
• 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

Description

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).

Biochem/physiol Actions

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

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.

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 10-13 - German Storage Class 10 to 13