|
|
| | 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]- Basic information |
| | 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]- Chemical Properties |
| density | 1+-.0.1 g/cm3(Predicted) | | pka | 4.46±0.10(Predicted) |
| | 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]- Usage And Synthesis |
| 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 |
| | 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]- Preparation Products And Raw materials |
|