Devimistat (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 Experiment | |
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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. |
Concentrations | 100 µM |
Incubation time | 6 h |
Animal Experiment | |
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Animal models | CD1-Nu/Nu female mice |
Formulation | PBS |
Dosages | 25 mg/kg |
Administration | i.p. |
Molecular Weight | 388.59 |
Formula | C22H28O2S2 |
CAS Number | 95809-78-2 |
Solubility (25°C) | DMSO 48 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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