AZ-5104
Cat. No.:YN340253
CAS No. :1421373-98-9
产品名称: | AZ-5104 |
CAS No.: | 1421373-98-9 |
Chemical Name: | N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide |
Synonyms: | AZ5104;AZ-5104;AZD5104;AZ 5104;IQNVEOMHJHBNHC-UHFFFAOYSA-N;AOB87166;BCP08428;BDBM50029689;s7298;BC600726;AK174234;B5836;N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide;N-(2-[2-Dimethylamin |
分子量: | 485.58 |
分子式: | C₂₇H₃₁N₇O₂ |
SMILES: | C=CC(NC1=CC(NC2=NC=CC(C3=CNC4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O |
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: | AZ-5104是AZD 9291的活性,去甲基化代谢物。AZ-5104是EGFR抑制剂;抑制EGFRL858R/T790M,EGFRL858R,EGFRL861Q,EGFR 和ErbB4的IC50值分别为1,6,1,25和7 nM。 |
IC50和靶点: | [{name:"EGFRL858R/T790M:1 nM (IC50)"},{name: "EGFRL858R:1 nM (IC50)"},{name: "EGFRL861Q:6 nM (IC50)"},{name: "EGFR:25 nM (IC50)"},{name: "ErbB4:7 nM (IC50)'}, 'EGFRExon 19 deletion/T790M'] |
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Finlay, M.R., Anderton, M., Ashton, S., et al.Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptorJ. Med. Chem.57(20),8249-8267(2014)
Dickinson, P.A., Vantarini, M.V., Collier, J., et al.Metabolic disposition of osimertinib in rats, dogs, and humans: Insights into a drug designed to bind covalently to a cysteine residue of epidermal growth factor receptorDrug Metab. Dispos.44(8),1201-1212(2016)