WZ4002

Biological Activity In vitro studies In vivo studies

Product Name: WZ4002
CAS No.: 1213269-23-8
Chemical Name: WZ4002
Synonyms: CS-166;WZ4002;WZ4002(HBr);WZ4002, >=98%;WZ4002 USP/EP/BP;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-methyl-1-piperazinyl)phen...;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)anilino]pyriMidin-4-yl]oxyphenyl]prop-2-enaMide
CBNumber: CB52501012
Molecular Formula: C25H27ClN6O3
Formula Weight: 494.97
MOL File: 1213269-23-8.mol

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WZ4002 Property

Density: 1.314
storage temp.: Store at -20°C
solubility: ≥24.7 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form: solid
pka: 12.78±0.70(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1168
Product name: WZ4002
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $74.1
Updated: 2024/03/01

Cayman Chemical

Product number: 16297
Product name: WZ4002
Purity: ≥98%
Packaging: 5mg
Price: $62
Updated: 2024/03/01

Cayman Chemical

Product number: 16297
Product name: WZ4002
Purity: ≥98%
Packaging: 10mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 16297
Product name: WZ4002
Purity: ≥98%
Packaging: 50mg
Price: $419
Updated: 2024/03/01

Cayman Chemical

Product number: 16297
Product name: WZ4002
Purity: ≥98%
Packaging: 100mg
Price: $714
Updated: 2024/03/01

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WZ4002 Chemical Properties,Usage,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.

Uses

WZ 4002 is an EGFR phosphorylation inhibitor.

Definition

ChEBI: WZ4002 is a pyrimidine compound having a 2-methoxy-4-(4-methylpiperazin-1-yl)anilino group at the 2-position, a 3-(acryloylamino)phenoxy group at the 4-position, and a chloro substituent at the 5-position. It has a role as a tyrosine kinase inhibitor and an antineoplastic agent. It is a member of pyrimidines, a member of piperazines and an organochlorine compound.

Biological Activity

wz4002 is a novel mutant-selective epidermal growth factor receptor (egfr) kinase inhibitor that potently and irreversibly suppresses the atp-dependent auto-phosphorylation of both wild-type egfr and egfr mutants, including egfr dele746_a750/t790m, egfr l858r/t790m, egfr t790m, egfr dele746_a750 and egfr l858r, with inhibition constant ki of 13.6 nm, 1.8 nm, 4 nm, 5 nm, 3.9 nm and 8.5 nm respectively. although wz4002 is actively against egfr mutants rather than wild-type egfr at lower concentrations resulting in less toxicity in normal tissues, wild-type egfr is susceptible to higher concentrations of wz4002 as well as prolonged administration of wz4002, especially in tissues where it accumulates.

target

EGFRL858R

storage

Store at -20°C

References

[1]lee hj, schaefer g, heffron tp, shao l, ye x, sideris s, malek s, chan e, merchant m, la h, ubhayakar s, yauch rl, pirazzoli v, politi k, settleman j. noncovalent wild-type-sparing inhibitors of egfr t790m. cancer discov. 2013 feb;3(2):168-81. doi: 10.1158/2159-8290.cd-12-0357. epub 2012 dec 10.
[2]zhou w, ercan d, chen l, yun ch, li d, capelletti m, cortot ab, chirieac l, iacob re, padera r, engen jr, wong kk, eck mj, gray ns, jänne pa. novel mutant-selective egfr kinase inhibitors against egfr t790m. nature. 2009 dec 24;462(7276):1070-4. doi: 10.1038/nature08622.
[3]zannetti a, iommelli f, speranza a, salvatore m, del vecchio s. 3'-deoxy-3'-18f-fluorothymidine pet/ct to guide therapy with epidermal growth factor receptor antagonists and bcl-xl inhibitors in non-small cell lung cancer. j nucl med. 2012 mar;53(3):443-50. doi: 10.2967/jnumed.111.096503. epub 2012 feb 13.

WZ4002 Preparation Products And Raw materials

Raw materials

Preparation Products

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WZ4002 Suppliers

China 178 China Hong Kong 1 India 1 United States 21 Global 201

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View Lastest Price from WZ4002 manufacturers

Henan Aochuang Chemical Co.,Ltd.

Product: WZ4002 1213269-23-8
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1ton
Release date: 2022-09-22

Zhejiang J&C Biological Technology Co.,Limited

Product: WZ4002 1213269-23-8
Price: US $0.00/gram
Min. Order: 1gram
Purity: 99%
Supply Ability: 10kg
Release date: 2022-02-17

Shijiazhuang tongyang Import and Export Co., LTD

Product: WZ4002 1213269-23-8
Price: US $10.00/KG
Min. Order: 1g
Purity: 99
Supply Ability: 100kg/kg
Release date: 2021-08-11

1213269-23-8, WZ4002Related Search:

BKM-120 WZ8040 WZB117 WZ4141 AP26113 Lenvatinib Afatinib (BIBW 2992) Vandetanib Gefitinib Alisertib (MLN8237) Erlotinib hydrochloride Capmatinib Ceritinib (LDK378) Selumetinib Cabozantinib Dabrafenib Dacomitinib (PF299804) WZ4141R

WZ4002

CS-166

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-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

N-[3-[5-chloro-2-[2-Methoxy-4-(4-Methylpiperazin-1-yl)anilino]pyriMidin-4-yl]oxyphenyl]prop-2-enaMide

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

2-Propenamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-

WZ4002 USP/EP/BP

N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide hydrobromide

N-{3-[(5-Chloro-2-{[2-methoxy-4-(4-methyl-1-piperazinyl)phen...

N-[3-[[5-Chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide HBr

1213269-23-8

213269-23-8

123269-23-6

3269-23-8

C25H27ClN6O3

api

Inhibitors

WZ4002 is an EGFR T790M inhibitor(IC50<20nM).