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PFK-158
产品别名
1462249-75-7
PFK-158
PFK 158
(2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one
(E)-1-(Pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one
PFK158
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H11F3N2O |
| Molecular weight | 328.29 |
| MDL number | MFCD28386154 |
| Biochem/physiol Actions【生化/生理作用】 | PFK158 is a 3PO analog with improved PFKFB3 inhibitory potency (cell-free IC50 = 137 nM; Jurkat cellular IC50 = 1.62 μM/PFKFB3 activity, 847 nM/2-deoxyglucose uptake, 328 nM/toxicity) and pharmacokinetic properties. PFK158 markedly sensitizes BRAF(V600E)-positive A375 melanoma cells to apoptosis induction by vemurafenib in cultures and causes ~80% growth inhibition in several murine models of human-derived tumors in vivo (60 mg/kg qod. ip.). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear (warmed) |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=C(/C=C/C1=NC2=C(C=CC(C(F)(F)F)=C2)C=C1)C3=CC=NC=C3 |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
