Cat No.
CEI-0049
Description
Neratinib (HKI-272) can inhibit HER2 and EGFR with IC50 of 59 nM and 92 nM.
CAS No.
698387-09-6
Targets
HER2, EGFR
Chemical Name
(E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide
M.Wt
557.04
Purity
>99%
Solubility
DMSO 2 mg/mL Water
Storage
2 years at -20centigrade Powder
In vitro
Neratinib (HKI-272) can inhibit HER2, a member of ErbB family of receptor tyrosine kinases, with IC50 of 59 nM. Neratinib (HKI-272) also shows inhibition to EGFR with IC50 of 97 nM. HKI-272 repressed the proliferation of a mouse fibroblast cell line (3T3) transfected with the HER-2 oncogene (3T3/ neu) with IC50 of 3 nM, and neratinib (HKI-272) shows a high degree of selectivity for this oncogenic pathway. HKI-272 also inhibited two other HER-2-overexpressing breast cancer cell lines, SK-Br-3 and BT474 with IC50 of 2 nM.
In vivo
The maximum tolerated dose of once-daily oral neratinib is 320 mg. The most common neratinib-related toxicity was diarrhea.
