WZ4002
Cat. No.：YN340096
CAS No. ：1213269-23-8
| 产品名称: | WZ4002 |
| CAS No.: | 1213269-23-8 |
| Chemical Name: | N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide |
| Synonyms: | WZ4002,WZ 4002,WZ-4002 |
| 分子量: | 494.97 |
| 分子式: | C₂₅H₂₇ClN₆O₃ |
| SMILES: | COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C(C(OC4=CC(NC(C=C)=O)=CC=C4)=N3)Cl |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | WZ4002是突变选择性的EGFR抑制剂；对EGFRL858R，EGFRL858R/T790M，EGFRE746_A750，EGFRE746_A750/T790M的IC50值分别为2，8，3，2 nM。 |
| IC50和靶点: | [{name:"EGFRL858R:2 nM (IC50, Cell Assay)"},{name: "EGFRL858R/T790M:8 nM (IC50, Cell Assay)"},{name: "EGFRE746_A750:3 nM (IC50, Cell Assay)"},{name: "EGFRE746_A750/T790M:2 nM (IC50, Cell Assay)"}] |
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| Solvent & Solubility: |
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Zhou, W., Ercan, D., Chen, L., et al.Novel mutant-selective EGFR kinase inhibitors against EGFR T790MNature462(7276),1070-1074(2009)
Lee, H.J., Schaefer, G., Heffron, T.P., et al.Noncovalent wild-type-sparing inhibitors of EGFR T790MCancer Discov.3(2),168-181(2013)
Wang, W., Li, Q., Takeuchi, S., et al.Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancerClin. Cancer Res.18(6),1663-1671(2012)
Nakagawa, T., Takeuchi, S., Yamada, T., et al.Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancerMol. Cancer Ther.11(10),2149-2157(2012)
Sakuma, Y., Yamazaki, Y., Nakamura, Y., et al.WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitorsLab. Invest.92(3),371-383(2012)
Nanjo, S., Yamada, T., Nishihara, H., et al.Ability of the Met kinase inhibitor crizotinib and new generation EGFR inhibitors to overcome resistance to EGFR inhibitorsPLoS One8(12),1-13(2013)
