Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
Neratinib (HKI-272)
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
Molecular Weight
557.04
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
HER2, EGFR
Molecular Formula
C30H29CLN603
Chemical Name
(E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide
Solubility
DMSO 2 mg/mL Water
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.
Download
Download Datasheet