| CAS NO: | 95809-78-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 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 | CPI613; CPI-613; Devimistat; CPI 613 Chemical Name: 6,8-bis(benzylthio)octanoic acid SMILES Code: O=C(O)CCCCC(SCC1=CC=CC=C1)CCSCC2=CC=CC=C2 |
| 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. Cell Assay: Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity. |
|---|---|
| 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. |
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