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 (240 μM) also induces both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells. Similarly, CPI-613 (10 mg/kg) also produces significant tumor growth inhibition of H460 human non-small cell lung carcinoma in mouse model.
|Cell lines||BxPC-3 human pancreatic tumor cells|
|Preparation method||BxPC-3 human pancreatic tumor cells were treated with 50 µM CPI-613 or sham treated (i.e., vehicle), whereas the non-transformed NIH-3T3 mouse fibroblast cells were treated with 100 µM CPI-613 or sham treatment (i.e., vehicle), for 6 hours. The duration of treatment with CPI-613 was based on a time course experiment which measured the time taken to induce death in 10-15% of the cells. At the end of the 6-hour treatment period, live cells were selected based on Trypan blue exclusion and quantified using a hemocytometer.|
|Incubation time||6 h|
|Animal models||CD1-Nu/Nu female mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Translational assessment of mitochondrial dysfunction of pancreatic cancer from in vitro gene microarray and animal efficacy studies, to early clinical studies, via the novel tumor-specific anti-mitochondrial agent, CPI-613.
Lee KC, et al. Ann Transl Med. Ann Transl Med. ;2(9):91. PMID: 25405166.
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.
Lee KC, et al. Drug Metab Lett. 2011 Aug;5(3):163-82. PMID: 21722089.
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