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      Devimistat (CPI-613)
      Devimistat (CPI-613)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0853
      CAS #: 95809-78-2Purity ≥98%

      Description: Devimistat (formerly also known as CPI-613), a synthetic lipoate analog, is a novel and potent inhibitor of pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, it disrupts mitochondrial metabolism and shows strong antitumor activity. Devimistat inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, it disrupts tumor cell mitochondrial metabolism. Devimistat has potential chemopreventive and antineoplastic activities. CPI-613 is developed to target the pyruvate dehydrogenase complex which is a key mitochondrial enzyme of anaerobic glycolysis in tumor cells. 

      References: J Mol Med (Berl). 2011 Nov;89(11):1137-48.

      Related CAS #: 95809-78-2  

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      Molecular Weight (MW)388.59
      FormulaC22H28O2S2
      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
      SynonymsCPI613; CPI-613; Devimistat; CPI 613 

      Chemical Name: 6,8-bis(benzylthio)octanoic acid

      InChi Key: ZYRLHJIMTROTBO-UHFFFAOYSA-N

      InChi Code: InChI=1S/C22H28O2S2/c23-22(24)14-8-7-13-21(26-18-20-11-5-2-6-12-20)15-16-25-17-19-9-3-1-4-10-19/h1-6,9-12,21H,7-8,13-18H2,(H,23,24)

      SMILES Code: O=C(O)CCCCC(SCC1=CC=CC=C1)CCSCC2=CC=CC=C2           

      A

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      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 VivoCPI-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 modelCD1 nu/nu mice bearing BxPC-3 and H460 cells tumor models
      Formulation & DosageDissolved in DMSO and then diluted in water.; 25 mg/kg; i.p. administration
      ReferencesJ Mol Med (Berl). 2011 Nov;89(11):1137-48.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

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