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]

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 Conditions Sponsor/Collaborators Start Date Phases
NCT03699319 Not yet recruiting Pancreatic Cancer Jeffrey Hardacre|Case Comprehensive Cancer Center November 27 2018 Phase 2
NCT03374852 Withdrawn Pancreatic Ductal Adenocarcinoma Sidney Kimmel Cancer Center at Thomas Jefferson University|Rafael Pharmaceuticals Inc.|Thomas Jefferson University August 2018 Phase 2
NCT03370159 Withdrawn Stage IIIB Non-Small Cell Lung Cancer AJCC v7|Stage IV Non-Small Cell Lung Cancer AJCC v7 Wake Forest University Health Sciences|National Cancer Institute (NCI) June 2018 Phase 1|Phase 2
NCT01520805 Withdrawn Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Rafael Pharmaceuticals Inc. January 2016 Phase 2
NCT02168907 Terminated B-cell Adult Acute Lymphoblastic Leukemia|B-cell Chronic Lymphocytic Leukemia|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Testicular Lymphoma|Waldenström Macroglobulinemia Wake Forest University Health Sciences|National Cancer Institute (NCI) December 2014 Phase 1
NCT02232152 Recruiting Mucinous Adenocarcinoma of the Colon|Mucinous Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Signet Ring Adenocarcinoma of the Colon|Signet Ring Adenocarcinoma of the Rectum|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Wake Forest University Health Sciences|National Cancer Institute (NCI) December 2014 Phase 1

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.

Handling Instructions

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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