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| | Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- Basic information |
| | Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- Chemical Properties |
| Boiling point | 719.9±70.0 °C(predicted) | | density | 1.54±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | | pka | 9.02±0.20(predicted) |
| | Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- Usage And Synthesis |
| Uses | EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFRL858R/T790M/C797S and BaF3–C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models[1]. | | References | [1] Yao H, et al., Discovery of new cyclopropane sulfonamide derivatives as EGFR inhibitors to overcome C797S-mediated resistance and EGFR double mutation. Eur J Med Chem. 2024 Jun 16;275:116590. DOI:10.1016/j.ejmech.2024.116590 |
| | Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- Preparation Products And Raw materials |
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