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.
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Choose Selective Dehydrogenase Inhibitors
|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.|
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. 
|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. |
|In vitro||DMSO||77 mg/mL (198.15 mM)|
|Ethanol||77 mg/mL (198.15 mM)|
|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.
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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|NCT03374852||Withdrawn||Pancreatic Ductal Adenocarcinoma||Sidney Kimmel Cancer Center at Thomas Jefferson University|Rafael Pharmaceuticals Inc.|Thomas Jefferson University||August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|NCT03370159||Withdrawn||Stage IIIB Non-Small Cell Lung Cancer AJCC v7|Stage IV Non-Small Cell Lung Cancer AJCC v7||Wake Forest University Health Sciences|National Cancer Institute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|NCT01520805||Withdrawn||Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS)||Rafael Pharmaceuticals Inc.||January 2016||Phase 2|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|
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
How to dissolve the compund for in vivo applications?
CPI-613 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30mg/ml is a suspension, and it is for oral gavage.