CPI-613

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.
Targets
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]

Assay
Methods Test Index PMID
Western blot
pE1α; 

PubMed: 25165100     


PDH phosphorylation is increased by CPI-613. K562 cells were incubated with the indicated amount of CPI-613 as in A and harvested for lysates. Western blots for phospho-E1α were performed. Actin was blotted to serve as a loading control.

p-AMPK / AMPK ; 

PubMed: 25165100     


AMPK phosphorylation is increased by CPI-613. OCI-AML3 cells were incubated with the indicated amount of CPI-613 as in A and harvested for lysates. Western blots for phosphorylated AMPK (pAMPK) were performed. Total AMPK (tAMPK) was blotted to serve as a loading control.

25165100
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]

Protocol

Animal Research:[1]
+ Expand
  • 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.
14mg/mL

* 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
Formula

C22H28O2S2

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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03793140 Recruiting Drug: CPI-613 Lymphoma|Leukemia Memorial Sloan Kettering Cancer Center|City of Hope Medical Center|Massachusetts General Hospital|M.D. Anderson Cancer Center|George Washington University December 31 2018 Phase 2
NCT01902381 Suspended Drug: 68-bis(benzylthio)octanoic acid Previously Treated Myelodysplastic Syndromes Wake Forest University Health Sciences|National Cancer Institute (NCI) August 2013 Phase 2

Tech Support

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