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.
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. |
