WZ8040
Cat. No.：YN340299
| 产品名称: | WZ8040 |
| CAS No.: | 1214265-57-2 |
| Chemical Name: | N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide |
| Synonyms: | WZ-8040;WZ 8040 |
| 分子量: | 481.01384 |
| 分子式: | C24H25ClN6OS |
| SMILES: | O=C(C=C)NC1=CC=CC(SC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1 |
| 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: | WZ8040 是不可逆的、突变的EGFRT790M的抑制剂，可以抑制EGFR磷酸化。WZ8040 对突变型EGFR的活性是野生型EGFR 的100倍以上。 |
| IC50和靶点: | [{name:"EGFR Del E746_A750:1 nM (IC50, in HCC827 cells)"},{name: "EGFR Del E746_A750:6 nM (IC50, in PC9 cells)"},{name: "EGFR L858R:66 nM (IC50, in H3255 cells\r\r\r\r\r\r)"},{name: "EGFR L858R/T790M:9 nM (IC50, in H1975 cells)"},{name: "EGFR Del E746_A750/T790M:8 nM (IC50, in PC9 GR cells)"},{name: "EGFR E746_A750/MET amp:>3.3 μM (IC50, in HCC827 GR cells)"},{name: "ERBB2 amp:738 nM (IC50, in H1819 cells)"},{name: "ERBB2 amp:915 nM (IC50, in Calu-3 cells)"},{name: "ERBB2 Ins G776V, C:744 nM (IC50, in H1781 cells)"},{name: "EGFR & ERBB2 WT:1.82 μM (IC50, in HN11 cells)"}] |
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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)
Zhou, W., Ercan, D., Jänne, P.A., et al.Discovery of selective irreversible inhibitors for EGFR-T790MBioorg. Med. Chem. Lett.21(2),638-643(2011)
