| Identification | Back Directory | [Name]
Benzamide, N-[2-[2-[2-[2-[[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]- | [CAS]
2281803-28-7 | [Synonyms]
Benzamide, N-[2-[2-[2-[2-[[4-[2-(difluoromethyl)-1H-benzimidazol-1-yl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]- | [Molecular Formula]
C36H37F5IN9O6 | [MOL File]
2281803-28-7.mol | [Molecular Weight]
913.63 |
| Hazard Information | Back Directory | [Uses]
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines[1]. | [IC 50]
MEK1: 124 ± 11 nM (IC50); PI3Kα: 130 ± 13 nM (IC50); PI3Kδ: 236 ± 29 nM (IC50); PI3Kβ: 1537 ± 188 nM (IC50); PI3Kγ: 2745 ± 485 nM (IC50) | [References]
[1] Van Dort ME, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996. DOI:10.1016/j.ejmech.2021.113996 |
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