General description
A potent, cell-permeable, irreversible, ATP-competitive and selective inhibitor of EGF receptor (EGFR) tyrosine kinase activity (IC50 = 0.70 nM). Does not inhibit other protein kinases. Acts by binding to the catalytic domain of the EGFR with a 1:1 stoichiometry and alkylating Cys773. Excellent antitumor agent in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EGFR
Product competes with ATP.
Reversible: no
Target IC50: 700 pM against EGFR
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. Avoid freeze/thaw cycles of solutions.
Other Notes
Fry, D.W., et al. 1998. Proc. Natl. Acad. Sci USA 95, 12022.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 200 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | Brc1cc(ccc1)Nc2ncnc3c2cc(cc3)NC(=O)C=C |
| InChI | 1S/C17H13BrN4O/c1-2-16(23)21-13-6-7-15-14(9-13)17(20-10-19-15)22-12-5-3-4-11(18)8-12/h2-10H,1H2,(H,21,23)(H,19,20,22) |
| InChI key | HTUBKQUPEREOGA-UHFFFAOYSA-N |
