CL 387,785

Overactivity of epidermal growth factor receptor (EGFR) tyrosine kinase activity has been associated with a number of cancers. CL 387,785 is a potent, irreversible inhibitor of EGFR kinase activity (IC50 = 370 pM). It blocks EGF-stimulated autophosphorylation of receptors in cells (IC50 = 5 nM) and halts cell cycling in cells that overexpress EGFR or c-ErbB2 (IC50s = 31-125 nM). CL 387,785 profoundly blocks the growth of EGFR-overexpressing tumors in nude mice when given orally at 80 mg/kg/day for 10 days.Formal Name: N-[4-[(3-bromophenyl)amino]-6-quinazolinyl]-2-butynamide. CAS Number: 194423-06-8. Synonyms: EKB-785, EKI-785, WAY-EKI-785. Molecular Formula: C18H13BrN4O. Formula Weight: 381.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 5 mg/ml. lambdamax: 246, 317, 348 nm. SMILES: BrC1=CC(NC2=NC=NC3=C2C=C(NC(C#CC)=O)C=C3)=CC=C1. InChi Code: InChI=1S/C18H13BrN4O/c1-2-4-17(24)22-14-7-8-16-15(10-14)18(21-11-20-16)23-13-6-3-5-12(19)9-13/h3,5-11H,1H3,(H,22,24)(H,20,21,23). InChi Key: BTYYWOYVBXILOJ-UHFFFAOYSA-N.