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Submit ReviewVER 246608
说明： Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3/4 inhibitor
化学名： N-[4-(2-Chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
纯度： ≥98% (HPLC)
生物活性 for VER 246608
VER 246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK; IC50s = 35, 40, 84, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4 respectively). It is selective for PDKs over a panel of 97 kinases and HSP90. VER 246608 increases pyruvate dehydrogenase complex activity, oxygen consumption and reduces glycolytic activity; it reduces the production of L-lactate in PC3 cells in D-glucose and L-glutamine depleted media. In PC3 cells, VER 246608 induces cell cycle arrest at the G1 phase under glucose or serum-depleted conditions characteristic of the tumor microenvironment.
化合物库 for VER 246608
VER 246608 is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for VER 246608
| 分子量 | 552.96 |
| 公式 | C28H23ClF2N4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1684386-71-7 |
| PubChem ID | 86280454 |
| InChI Key | LCGNLQSOSJFLKR-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=C(O)C=C1O)N(C=2C=CC(=CC2)C3=NC(Cl)=NC=C3C)CC4=CC=C(C=C4)CNC(=O)C(F)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VER 246608
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 55.3 | 100 |
制备储备液 for VER 246608
以下数据基于产品分子量 552.96。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.81 mL | 9.04 mL | 18.08 mL |
| 5 mM | 0.36 mL | 1.81 mL | 3.62 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.81 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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产品说明书 for VER 246608
参考文献 for VER 246608
参考文献是支持产品生物活性的出版物。
Brough et al (2017) Application of off-rate screening in the identification of novel pan- isoform inhibitors of pyruvate dehydrogenase kinase. J.Med.Chem. 60 2271 PMID: 28199108
Moore et al (2014) VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget 5 12862 PMID: 25404640
If you know of a relevant reference for VER 246608, please let us know.
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关键词: VER 246608, VER 246608 supplier, VER246608, pan-isoform, ATP, competitive, inhibitor, inhibits, pyruvate, dehydrogenase, kinase, PDK, PDHK, cancer, metabolism, tumor, microenvironment, Other, Kinases, 6604, Tocris Bioscience
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