CAS:95809-78-2CPI-613

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CPI-613 CPI-613 Cat No. FB08313Cas No. 95809-78-2

Synonyms: 6,8-Bis(benzylthio)octanoic acid

CPI-613 is an E1α pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. CPI-613 has been granted orphan drug status by the US FDA for pancreatic cancer.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5734 mL
- 12.8671 mL
- 25.7343 mL
- 5 mM
- 0.5147 mL
- 2.5734 mL
- 5.1469 mL
- 10 mM
- 0.2573 mL
- 1.2867 mL
- 2.5734 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

95809-78-2

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C22H28O2S2

运输

蓝冰

分子量

388.59

别名

6,8-Bis(benzylthio)octanoic acid

溶解度

DMSO	150.0 mg/mL (386.0 mM)
Water	insoluble

动物实验配方

靶点数据

生物活性

描述CPI-613 is a novel anti-tumor compound targeting on PDH. CPI-613 at concentration of 240μM disrupted H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity, and caused loss of mitochondrial membrane potential. It induced extensive post-translational modification of PDH E1 at 300μM, which is acquired high PDK levels. CPI-613 demonstrated anticancer activity both in vitro and in vivo. It induced both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells at concentration of 240μM in 22 or 24h. It showed strong antitumor activity against human non-small cell lung and pancreatic cancers in xenograft models at dose of 25mg/kg. CPI-613 undergoes both phase 1 (oxidation) and phase 2 (glucuronidation) transformations. Inhibition of KGDH by CPI-613 may partially contribute to antitumor activity of CPI-613. It inhibited KGDH function strongly and rapidly, selectively in tumor cells. Moreover, CPI-613 induced a correspondingly rapid, powerful redox signal in tumor cell mitochondria.
动物研究
剂量
Mice: 25 mg/kg^[4] (i.p.), 100 mg/kg^[1] (i.p., MTD)

给药途径
i.p.

动物研究
剂量	Mice: 25 mg/kg^[4] (i.p.), 100 mg/kg^[1] (i.p., MTD)
给药途径	i.p.