EGFR Inhibitor

EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells. It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 µM). Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.Formal Name: N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide. CAS Number: 879127-07-8. Synonyms: Epidermal Growth Factor Receptor Inhibitor, ErbB-1 Inhibitor, HER1 Inhibitor. Molecular Formula: C21H18F3N5O. Formula Weight: 413.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 253, 302 nm. SMILES: O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2. InChi Code: InChI=1S/C21H18F3N5O/c22-21(23,24)14-3-1-4-15(9-14)27-18-11-19(26-12-25-18)28-16-5-2-6-17(10-16)29-20(30)13-7-8-13/h1-6,9-13H,7-8H2,(H,29,30)(H2,25,26,27,28). InChi Key: YOHYSYJDKVYCJI-UHFFFAOYSA-N.