Cayman 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.^,

WARNING This product is not for human or veterinary use.