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CPI-613

Cat. No. M2297
CPI-613 Structure
Size Price Availability Quantity
10mg USD 75 In stock
50mg USD 160 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Stem Cells Dev (2017). Figure 8. CPI-613
Method Amplex Ultra Red (AUR) assay
Cell Lines KGDHC and PDHC
Concentrations 10 μM
Incubation Time 15 min
Results At lower concentrations, KMV was not as effective as CPI-613 at suppressing ROS formed by pyruvate metabolism. This is in contrast to mitochondria oxidizing α- ketoglutarate where KMV and CPI-613 elicited similar effects.
Source Stem Cells Dev (2017). Figure 5. CPI-613
Method Amplex Ultra Red (AUR) assay
Cell Lines KGDHC and PDHC
Concentrations 150 μM
Incubation Time 15 min
Results It had been previously shown that 150 μM CPI-613 is effective at inhibiting PDHC and KGDHC. It is important to emphasize that albumin needs to be excluded from reaction mixtures since it can interfere with the CPI-613 mediated inhibition of PDHC or KGDHC.
Protocol
Cell Experiment
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
Animal models CD1-Nu/Nu female mice
Formulation PBS
Dosages 25 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 388.59
Formula C22H28O2S2
CAS Number 95809-78-2
Purity 99.78%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CPI-613 supplier, Dehydrogenase, inhibitors

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