Neratinib (HKI-272)

inquiry

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.

Name:

Email *

Phone:*

Company/Institution:

Country or Region:

Quantity:

Services & Products Interested *

Project Description:

Our Products Cannot Be Used As Medicines Directly For Personal Use.

Products

Online Inquiry