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| Product Name: | WZ8040 | | Synonyms: | WZ8040;N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide;CS-471;N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide;N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide WZ8040;N-(3-((5-Chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylami;WZ-8040;WZ 8040;2-Propenamide, N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]- | | CAS: | 1214265-57-2 | | MF: | C24H25ClN6OS | | MW: | 481.01 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1214265-57-2.mol |  |
| | WZ8040 Chemical Properties |
| density | 1.37 | | storage temp. | Store at -20°C | | solubility | ≥24.05 mg/mL in DMSO; insoluble in H2O; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic | | form | solid | | pka | 12.94±0.70(Predicted) |
| | WZ8040 Usage And Synthesis |
| Description | WZ8040 is an inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 306 nM in Ba/F3 cells. It is selective for EGFR mutants, including the EGFRDel E746_A750 and EGFRL858R mutations conferring gefitinib sensitivity and the EGFRDel E746_A750/T790M mutation conferring gefitinib resistance (IC50s = 2, 6, and 6 nM in Ba/F3 cells), over wild-type EGFR (IC50 = 1,820 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 20 and 32 nM, respectively, in Ba/F3 cells). WZ8040 inhibits proliferation of PC-9 cells harboring the EGFRDel E746_A750 mutation and gefitinib-resistant PC-9 GR cells harboring the EGFRT790M resistant allele (EC50s = 6 and 8 nM, respectively). | | Uses | WZ8040 is an irreversiblely EGFR T790M inhibitor (IC50<10nM). | | target | EGFR T790M | | references | [1] zhou w1, 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. |
| | WZ8040 Preparation Products And Raw materials |
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