1684386-71-7
1684386-71-7 性质
| 沸点 | 830.4±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.414±0.06 g/cm3(Predicted) |
| 溶解度 | DMF:2.0(最大浓度 mg/mL);3.62(最大浓度 mM) DMSO:2.0(最大浓度 mg/mL);3.62(最大浓度 mM) DMSO:PBS ( pH 7.2) (1:1):0.5(最大浓度 mg/mL);0.9(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 7.61±0.35(Predicted) |
1684386-71-7 用途与合成方法
IC50: 35 nM (PDK-1), 40 nM (PDK-3), 84 nM (PDK-2), 91 nM (PDK-4)
VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK. VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range. In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser 293 residue of E1α (phosphorylated by all four PDK isozymes) with IC 50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth.
1684386-71-7 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-12492 | 1684386-71-7 | 1684386-71-7 | 1mg | 636 |
| 2024-01-25 | HY-12492 | 1684386-71-7 | 1684386-71-7 | 5mg | 1400 |
