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product name CPI-613


Description: CPI-613, a synthetic lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, it disrupts tumor cell mitochondrial metabolism. CPI-613 has potential chemopreventive and antineoplastic activities. CPI-613 is developed to target the pyruvate dehydrogenase complex which is a key mitochondrial enzyme of anaerobic glycolysis in tumor cells.

References: J Mol Med (Berl). 2011 Nov;89(11):1137-48.



Molecular Weight (MW)

388.59
Formula

C22H28O2S2
CAS No.

95809-78-2
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 78 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 78 mg/mL (200.7 mM)
Solubility (In vivo)

 1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19409876

In Vitro

In vitro activity:In vitro, CPI-613 produces the selective toxicity against several tumor cell lines including H460 human lung cancer cells and Saos-2 human sarcoma cells with EC50 of 120 μM and 120 μM, respectively. CPI-613 disrupts H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity and loss of mitochondrial membrane potential in a time- and drug dose-dependent fashion. In addition, CPI-613 (240 μM) also induces both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells.


Kinase Assay


Cell Assay

In Vivo CPI-613 (25 mg/kg) has potent anticancer activity in a human tumor xenograft model of of a pancreatic tumor cell (BxPC-3). Similarly, CPI-613 (10 mg/kg) also produces significant tumor growth inhibition of H460 human non-small cell lung carcinoma in mouse model. Besides, CPI-613 produces little or no side-effect toxicity in expected therapeutic dose ranges in large animal models and has the maximum tolerated dose of 100 mg/kg in mice.
Animal model CD1 nu/nu mice bearing BxPC-3 and H460 cells tumor models
Formulation & Dosage Dissolved in DMSO and then diluted in water.; 25 mg/kg; i.p. administration
References J Mol Med (Berl). 2011 Nov;89(11):1137-48.

MK-0773

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Author: Sodium channel