| Identification | Back Directory | [Name]
2-Propenamide, N-[2-[2-[(dimethylamino)methyl]-1H-pyrrol-1-yl]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]- | [CAS]
2413958-04-8 | [Synonyms]
EGFR kinase inhibitor 1
2-Propenamide, N-[2-[2-[(dimethylamino)methyl]-1H-pyrrol-1-yl]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]- | [Molecular Formula]
C30H31N7O2 | [MOL File]
2413958-04-8.mol | [Molecular Weight]
521.61 |
| Hazard Information | Back Directory | [Uses]
EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1]. | [IC 50]
EGFR (WT): 37 nM (IC50); EGFRL858R/T790M: 1.7 nM (IC50); EGFRL858R/T790M/C797S: >300 nM (IC50) | [References]
[1] Ding S, et al. Design, synthesis and biological evaluation of novel N-(3-amino-4-methoxyphenyl)acrylamide derivatives as selective EGFRL858R/T790M kinase inhibitors. Bioorg Chem. 2022 Jan;118:105471. DOI:10.1016/j.bioorg.2021.105471 |
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