
Cellagen Technology
EGFR, Her2 inhibitor
BIBW2992 (Afatinib) is an orally-available, aminoquinazoline-acrylamide-based inhibitor with IC50 potency for EGFRwt, EGFR(L858R), EGFR(L858R/T790M), and HER2 at 0.5, 0.4, 10, and 14 nM, respectively. [1] Via its crotonamide functional group, BIBW2992 targets the ErbB family in an irreversible manner, providing a sustained, selective, and covalent inhibition that has been shown to be effective toward erlotinib-resistant tumors. [2]
In cellular assays, BIBW2992 inhibits phosphorylation of EGFR wild type (A431), EGFR (NCI-H1975), and HER2 (BT474) at EC50s of 8, 49, and 75 nM, respectively. [3]
BIBW2992 displays potent growth inhibition of EGFR/HER2 expressing lung cancer cell lines H1666, H3255, and NCI1975 at IC50 values of 60, 0.7, and 99 nM, respectively. [1]




Cellagen Technology
EGFR, Her2 inhibitor


BIBW2992 (Afatinib) is an orally-available, aminoquinazoline-acrylamide-based inhibitor with IC50 potency for EGFRwt, EGFR(L858R), EGFR(L858R/T790M), and HER2 at 0.5, 0.4, 10, and 14 nM, respectively. [1] Via its crotonamide functional group, BIBW2992 targets the ErbB family in an irreversible manner, providing a sustained, selective, and covalent inhibition that has been shown to be effective toward erlotinib-resistant tumors. [2]
In cellular assays, BIBW2992 inhibits phosphorylation of EGFR wild type (A431), EGFR (NCI-H1975), and HER2 (BT474) at EC50s of 8, 49, and 75 nM, respectively. [3]
BIBW2992 displays potent growth inhibition of EGFR/HER2 expressing lung cancer cell lines H1666, H3255, and NCI1975 at IC50 values of 60, 0.7, and 99 nM, respectively. [1]