Products

Enzymes for Research, Diagnostic and Industrial Use

WZ8040

Cat No.
CEI-0854
Description
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
CAS No.
1214265-57-2
Molecular Weight
481.01
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
EGFR L858R, EGFR E746_A750, EGFR L858R/T790M, EGFR E746_A750/T790M
Molecular Formula
C24H25ClN6OS
Chemical Name
N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide
Solubility
DMSO 96 mg/mL; Water <1 mg/mL; Ethanol 3 mg/mL
In vitro
WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells.
Download Datasheet:



Inquiry
Realted Products
Catalog
ProductName
EC No.
CAS No.
Source
Price
CatalogCEI-0013
ProductNameOSI-420
EC No.
CAS No.183320-51-6
Source
CatalogCEI-0014
ProductNameWZ4002
EC No.
CAS No.1213269-23-8
Source
CatalogCEI-0016
ProductNamePD153035 HCL
EC No.
CAS No.183322-45-4
Source
CatalogCEI-0018
ProductNameLapatinib
EC No.
CAS No.231277-92-2
Source
+ See More >>
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: