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Chemical Structure| 95809-78-2 同义名 : 6,8-双(苄基硫基)辛酸 ;CPI-613
CAS号 : 95809-78-2
货号 : A158224
分子式 : C22H28O2S2
纯度 : 98%
分子量 : 388.587
MDL号 : MFCD22420826
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(270.21 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Dehydrogenase
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[4]. CPI-613 undergoes both phase 1 (oxidation) and phase 2 (glucuronidation) transformations[5]. 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[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.73mL

5.15mL

2.57mL
参考文献

[1]Zachar Z, Marecek J, et al. Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo. J Mol Med (Berl). 2011 Nov;89(11):1137-48.

[2]Lee KC, Shorr R, et al. Formation and anti-tumor activity of uncommon in vitro and in vivo metabolites of CPI-613, a novel anti-tumor compound that selectively alters tumor energy metabolism. Drug Metab Lett. 2011 Aug;5(3):163-82.

[3]Stuart SD, Schauble A, et al. A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process. Cancer Metab. 2014 Mar 10;2(1):4.

[4]Zachar Z, Marecek J, Maturo C, Gupta S, Stuart SD, Howell K, Schauble A, Lem J, Piramzadian A, Karnik S, Lee K, Rodriguez R, Shorr R, Bingham PM. Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo. J Mol Med (Berl). 2011 Nov;89(11):1137-48. doi: 10.1007/s00109-011-0785-8. Epub 2011 Jul 19. PMID: 21769686.

[5]Lee KC, Shorr R, Rodriguez R, Maturo C, Boteju LW, Sheldon A. Formation and anti-tumor activity of uncommon in vitro and in vivo metabolites of CPI-613, a novel anti-tumor compound that selectively alters tumor energy metabolism. Drug Metab Lett. 2011 Aug;5(3):163-82. doi: 10.2174/187231211796904991. PMID: 21722089.

[6]Stuart SD, Schauble A, Gupta S, Kennedy AD, Keppler BR, Bingham PM, Zachar Z. A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process. Cancer Metab. 2014 Mar 10;2(1):4. doi: 10.1186/2049-3002-2-4. PMID: 24612826; PMCID: PMC4108059.