Catalog No.S2776

CPI-613 Chemical Structure

Molecular Weight(MW): 388.59

CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. Phase 2.

Size Price Stock Quantity  
In DMSO USD 170 In stock
USD 110 In stock
USD 770 In stock
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Biological Activity

Description CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase in NCI-H460 cell line, disrupts tumor cell mitochondrial metabolism. Phase 2.
PDH [1]
(NCI-H460 cells)
α-ketoglutarate dehydrogenase [1]
(NCI-H460 cells)
In vitro

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. [1]

In vivo CPI-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. [1]


Animal Research:[1]
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  • Animal Models: BxPC-3 and H460 cells are injected s.c. into the dorsal flank of CD1 nu/nu mice.
  • Formulation: CPI-613 is dissolved in DMSO and then diluted in water.
  • Dosages: ≤25 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.15 mM)
Ethanol 77 mg/mL (198.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.59


CAS No. 95809-78-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01520805 Withdrawn Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Cornerstone Pharmaceuticals, Inc. January 2016 Phase 2
NCT01830322 Withdrawn Metastatic Pancreatic Adenocarcinoma Cornerstone Pharmaceuticals, Inc. January 2014 Phase 2
NCT01832857 Terminated Cancer Cornerstone Pharmaceuticals, Inc. June 2013 Phase 2
NCT01768897 Completed Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Recurrent Adult Acute Myeloid Leukemia Wake Forest University Health Sciences|National Cancer Institute (NCI) January 2013 Phase 1
NCT01034475 Completed Advanced Hematologic Malignancies Wake Forest University Health Sciences March 2010 Phase 1
NCT00907166 Suspended Cancer|Pancreatic Cancer|Pancreatic Carcinoma Cornerstone Pharmaceuticals, Inc. May 2009 Phase 1|Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    How to dissolve the compund for in vivo applications?

  • Answer:

    CPI-613 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, and it is for oral gavage.

Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID