Description
BIBW 2992 maleate can inhibit EGFR(WT), EGFR(L858R), EGFR(L858R/T790M), and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C32H33ClFN5O11
Chemical Name
(S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide
Solubility
DMSO 97 mg/mL Water
In vitro
BIBW 2992 maleate is an anilino-quinazoline irreversible EGFR/HER2 inhibitor.BIBW 2992 maleate shows potent activity against wild-type and mutant forms of EGFR and HER2, similar to gefitinib in potency for L858R EGFR,but about 100-fold more active against the gefitinib-resistant L858R-T790M EGFR double mutant, with an IC 50 of 10 nM. BIBW 2992 maleate is furthermore comparable to lapatinib and canertinib for in vitro potency against HER2, with an IC 50 of 14 nM.
In vivo
In mouse models and human patients, combination of afatinib and cetuximab, an anti-EGFR antibody, shows effect and overcome acquired resistance. Iin vivo that afatinib plus cetuximab significantly inhibits HER2 phosphorylation.
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