产品描述:
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.{25289} 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).{25289} 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.{25291,25290}