Details:
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Product Name: |
WZ4002 |
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Synonyms: |
WZ4002;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 |
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CAS: |
1213269-23-8 |
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MF: |
C25H27ClN6O3 |
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MW: |
0 |
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EINECS: |
-0 |
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Product Categories: |
WZ4002 is an EGFR T790M inhibitor(IC50<20nM).;Inhibitors |
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Mol File: |
Mol File |
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WZ4002 Chemical Properties |
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WZ4002 Usage And Synthesis |
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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). |
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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. |
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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. |
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Usage |
A novel mutant-selective EGFR kinase inhibitor of EGFRL858R and EGFRL858R/T790M with IC50s of 2 nM and 8 nM, respectively. |
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WZ4002 Preparation Products And Raw materials
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HenNan sunlake enterprise corporation is located in Henan Province , The central plain of China , Which enjoys favorable geogeaphical position and convenient transportion, The com[any was established in june. 1998 , until now having more than 18 years experience in manufacturing & exporting chemical raw material .
Sunlake is a professional manufacturer engaged in producing and selling chemicals,including Organic & inorganic chemicals , pigments & Dyestuffs , Water treatment chemicals , Food & FEED additives and others . these products have been being well exported to europe , southeast Asia , the Middle East , Africa , South America and some other countries and areas.
We sincerely welcome foreign friends to visit our plant for cooperation. With the idea of "quality first,credit priority, Excellent service", We are highly acknowledged by customers for good quality and competitive price. More importantly , the company has a strong R & D team, who are professional engineers and scholars with Ph. D. .So we are confident to serve you better with our high - quality products and professional team.
We are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional wupplier in international market.
We welcome any serious inquiries from all customers of the world, and sincerely hope to cooperate with you for a brilliant future!