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WZ4002

Biological Activity In vitro studies In vivo studies
WZ4002
WZ4002 structure
CAS No.
1213269-23-8
Chemical Name:
WZ4002
Synonyms
CS-166;WZ4002;WZ4002(HBr);WZ4002, >=98%;WZ4002;WZ 4002; WZ-4002;WZ 4002 N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-;N-(3-(5-Chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acr;N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide;N-[3-[5-chloro-2-[2-Methoxy-4-(4-Methylpiperazin-1-yl)anilino]pyriMidin-4-yl]oxyphenyl]prop-2-enaMide;N-{3-[(5-Chloro-2-{[2-Methoxy-4-(4-Methyl-1-piperazinyl)phenyl]aMino}-4-pyriMidinyl)oxy]phenyl}acrylaMide
CBNumber:
CB52501012
Molecular Formula:
C25H27ClN6O3
Formula Weight:
494.99
MOL File:
1213269-23-8.mol

WZ4002 Properties

Density 
1.314
pka
12.78±0.70(Predicted)
FDA UNII
6BQ432Z61M

WZ4002 price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 16297 WZ4002 ≥98% 1213269-23-8 5mg $49 2020-06-24 Buy
Cayman Chemical 16297 WZ4002 ≥98% 1213269-23-8 10mg $88 2020-06-24 Buy
Cayman Chemical 16297 WZ4002 ≥98% 1213269-23-8 50mg $343 2020-06-24 Buy
Cayman Chemical 16297 WZ4002 ≥98% 1213269-23-8 100mg $588 2020-06-24 Buy

WZ4002 Chemical Properties,Uses,Production

Biological Activity

WZ4002 is a novel, mutant selective EGFR inhibitor. The IC50 is 2 nM/8 nM when it acts on IC50 of 2 nM/8 nM in EGFR (L858R)/(T790M), and it has no inhibitory effect on ERBB2 phosphorylation (T798I).

In vitro studies

WZ4002 also inhibit other EGFR genotypes. For instance, the IC50 is 2nM and 6nM respectively when it acts on E746_A750 and E746_A750/T790M. Besides, the IC50 is 32nM when it acts on wild-type EGFR. It could inhibit the phosphorylation of EGFR, AKT and ERK1/2 when it acts on non-small cell lung cancer (NSCLC). WZ4002 also could inhibit the phosphorylation of EGFR when it acts on NIH-3T3 cells expressing different EGFRT790M mutant alleles. The dissociation constant of kinase was 95% higher when in the test when WZ4002 involved than that in the test DMSO involved instead. Because in aniline substitution in the C2 WZ4002 could obtain a methoxy group when it acts on EGFR, thus it’s more effective when it acts on EGFR than WZ3146. Compared with the quinazoline inhibitors, the efficiency of WZ4002 is 100 times lower than when it acts on wild-type EGFR. The inhibitory effect of WZ4002 on EGFR kinase activity of recombinant L858R/T790M protein is much higher than restrainable wild-type EGFR’s. However HKI-272 and Gefitinib are happened to have opposite inhibitory effect compared with WZ4002. In addition, phosphorylation of EGFR in H1975 and HCC827 cells of anti-Src TKI could be completely inhibited by third-generation EGFR TKI and WZ4002.

In vivo studies

When treated with T790M mutant mouse model for 2 weeks and had been used to study the efficacy of WZ4002, it is found that treatment with WZ4002 resulted in more effective significant tumor regression compared to the control group. When treated with low dose WZ4002 and high dose WZ4002, it would resulted in a 26% and 36% decrease in average uptake respectively.

Uses

A novel mutant-selective EGFR kinase inhibitor of EGFRL858R and EGFRL858R/T790M with IC50s of 2 nM and 8 nM, respectively.

WZ4002 Preparation Products And Raw materials

Raw materials

Preparation Products


WZ4002 Suppliers

Global( 158)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Cangzhou Wanyou New Material Technology Co.,Ltd
18631714998
sales@czwytech.com CHINA 914 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 115 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24723 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 30045 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 968 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 35434 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com CHINA 47486 58
career henan chemical co
0086-371-86658258
0086-371-86658258 factory@coreychem.com CHINA 29643 58

View Lastest Price from WZ4002 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-12-26 WZ4002
213269-23-8
US $1.00 / KG 1KG 97%-99.9% 100kg Career Henan Chemical Co
2019-08-29 WZ4002
1213269-23-8
US $1.00 / KG 1KG 98% 200kg career henan chemical co
2019-04-19 WZ4002
1213269-23-8
US $1.00 / g 1g 99% 1000kgs Cangzhou Wanyou New Material Technology Co.,Ltd

1213269-23-8(WZ4002)Related Search:


  • N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide
  • N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide
  • WZ4002(HBr)
  • N-{3-[(5-Chloro-2-{[2-Methoxy-4-(4-Methyl-1-piperazinyl)phenyl]aMino}-4-pyriMidinyl)oxy]phenyl}acrylaMide
  • N-[3-[5-chloro-2-[2-Methoxy-4-(4-Methylpiperazin-1-yl)anilino]pyriMidin-4-yl]oxyphenyl]prop-2-enaMide
  • N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide WZ 4002
  • WZ 4002 N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide
  • 2-Propenamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-[1213269-23-8] WZ4002 HBr
  • WZ4002, >=98%
  • WZ 4002 N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-
  • N-(3-((5-chloro-2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)oxy)phenyl)acrylamide WZ 4002
  • WZ4002;WZ 4002; WZ-4002
  • N-(3-(5-Chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acr
  • CS-166
  • WZ4002
  • 1213269-23-8
  • 123269-23-6
  • 3269-23-8
  • 213269-23-8
  • C25H27ClN6O3
  • WZ4002 is an EGFR T790M inhibitor(IC50<20nM).
  • Inhibitors
  • api
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