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 individually and in order:
2% DMSO+corn oil
* 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.
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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|NCT01520805||Withdrawn||Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS)||Cornerstone Pharmaceuticals, Inc.||January 2016||Phase 2|
|NCT01830322||Withdrawn||Metastatic Pancreatic Adenocarcinoma||Cornerstone Pharmaceuticals, Inc.||January 2014||Phase 2|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|
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.