Octanoic acid, 6,8-bis[(phenylMethyl)thio]- CAS NO.95809-78-2

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In vitro, CPI-613 has selective toxicity against a variety of tumor cell lines, including H460 human lung cancer cells and Saos-2 human sarcoma cells, with EC50 of 120μM and 120μM, respectively. CPI-613 interferes with the mitochondrial metabolism of H460 cancer cells, including the inhibition of PDH complex activity and cell membrane potential loss in a time- and drug dose-dependent manner. In addition, in H460 human lung cancer cells and Saos-2 human sarcoma cells, CPI-613 (240μM) can also induce apoptotic and non-apoptotic Chemicalbook cell death. In vivo study CPI-613 (25mg/kg) has effective anticancer activity in a human xenograft model of pancreatic tumor cells (BxPC-3). Similarly, CPI-613 (10mg/kg) will also have a significant tumor growth inhibitory effect in the H460 human non-small cell lung cancer mouse model. In addition, CPI-613 produces little or no side effects in many animal models within the expected therapeutic dose range, and has a maximum tolerated dose of 100 mg/kg in mice.

Devimistat (CPI-613) is a Lipoate analog that inhibits the mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in the NCI-H460 cell line, and interferes with the mitochondrial metabolism of tumor cells. CPI-613 can induce apoptosis of pancreatic cancer cells. Phase 2.