| Identification | Back Directory | [Name]
Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- | [CAS]
3035639-05-2 | [Synonyms]
Cyclopropanesulfonamide, N-[2-[[5-bromo-2-[[4-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C25H30BrN7O2S | [MOL File]
3035639-05-2.mol | [Molecular Weight]
572.52 |
| Hazard Information | Back Directory | [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 |
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