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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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]

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
+ 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 78 mg/mL (200.72 mM)
Ethanol 78 mg/mL (200.72 mM)
Water <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 Conditions Sponsor/Collaborators Start Date Phases
NCT01520805 Not yet recruiting 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 Recruiting Cancer Cornerstone Pharmaceuticals, Inc. June 2013 Phase 2
NCT01768897 Active, not recruiting 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 Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) January 2013 Phase 1
NCT01034475 Completed Advanced Hematologic Malignancies Comprehensive Cancer Center of Wake Forest University March 2010 Phase 1
NCT00907166 Active, not recruiting Cancer|Pancreatic Cancer|Pancreatic Carcinoma Cornerstone Pharmaceuticals, Inc. May 2009 Phase 1|Phase 2

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Handling Instructions

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Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID