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About This Item
Empirical Formula (Hill Notation):
C17H11ClFN5O · 2.5H2O
CAS Number:
Molecular Weight:
400.79
UNSPSC Code:
12352200
Quality Segment
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
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
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)
Storage Class
10-13 - German Storage Class 10 to 13
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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