1684386-71-7
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- CAS号:
- 1684386-71-7
- 英文名:
- VER-246608
- 英文别名:
- VAR-246608;VER-246608;Inhibitor,VER 246608,PDHK,VER246608,VER-246608,Pyruvate dehydrogenase kinase,inhibit,PDH kinase;N-(4-(2-Chloro-5-methylpyrimidin-4-yl)phenyl)-N-(4-((2,2-difluoroacetamido)methyl)benzyl)-2,4-dihydroxybenzamide;N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide;Benzamide, N-[4-(2-chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxy-
- 中文名:
- 1684386-71-7
- 中文别名:
- 化合物VER-246608;N-[4-(2-氯-5-甲基-4-嘧啶基)苯基]-N-[[4-[[(2,2-二氟乙酰基)氨基]甲基]苯基]甲基]-2,4 -二羟基-苯甲酰胺
- CBNumber:
- CB83369665
- 分子式:
- C28H23ClF2N4O4
- 分子量:
- 552.96
- MOL File:
- 1684386-71-7.mol
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1684386-71-7化学性质
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沸点:
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830.4±65.0 °C(Predicted)
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密度:
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1.414±0.06 g/cm3(Predicted)
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溶解度:
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DMF:2.0(Max Conc. mg/mL);3.62(Max Conc. mM)
DMSO:2.0(Max Conc. mg/mL);3.62(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.9(Max Conc. mM)-
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形态:
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A solid
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酸度系数(pKa):
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7.61±0.35(Predicted)
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1684386-71-7性质、用途与生产工艺
VER-246608 是一种有效的，ATP 竞争性的丙酮酸脱氢酶激酶 (PDK) 抑制剂，抑制 PDK-1，PDK-3，PDK-2，和 PDK-4，IC50 分别为 35 nM，40 nM，84 nM 和 91 nM。
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
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-12492 | 1684386-71-7
VER-246608 | 1684386-71-7 | 1mg | 636元 |
| 2024/01/25 | HY-12492 | 1684386-71-7
VER-246608 | 1684386-71-7 | 5mg | 1400元 |
1684386-71-7, 1684386-71-7 相关搜索:
- C28H23ClF2N4O4
- 化合物VER-246608
- N-[4-(2-氯-5-甲基-4-嘧啶基)苯基]-N-[[4-[[(2,2-二氟乙酰基)氨基]甲基]苯基]甲基]-2,4 -二羟基-苯甲酰胺
- 1684386-71-7
- N-(4-(2-Chloro-5-methylpyrimidin-4-yl)phenyl)-N-(4-((2,2-difluoroacetamido)methyl)benzyl)-2,4-dihydroxybenzamide
- Inhibitor,VER 246608,PDHK,VER246608,VER-246608,Pyruvate dehydrogenase kinase,inhibit,PDH kinase
- VAR-246608
- Benzamide, N-[4-(2-chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxy-
- N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
- VER-246608