CPI-613

Catalog No.S2776

CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. Phase 2.

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In DMSO USD 170 In stock
USD 110 In stock
USD 770 In stock
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CPI-613 Chemical Structure

CPI-613 Chemical Structure
Molecular Weight: 388.59

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. Phase 2.
Targets PDH [1] α-ketoglutarate dehydrogenase [1]
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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

E1α phosphorylation Cells are seeded and grown overnight. Five dishes per test group are treated with CPI-613or solven. Cells are lysed in situ with 150 μL lysis buffer A [455 μL Zoom 2D protein solubilizer 1, 2.5μL 1M Tris base, 5μL 100X protease inhibitor cocktail; 5μL 2M DTT] and lysates from all five dishes are pooled in a 1.5 mL microfuge tube and sonicated on ice for 15 passes at 50% power. After a 10-minute incubation at room temperature, 2.5μL of dimethylacrylamide (DMA) are added and lysates are incubated for an additional 10 minutes. 5μL of 2 M DTT are added to neutralize excess DMA. Lysates are centrifuged for 15 minutes and the supernatant is recovered. Then, 40μL of lysate are mixed with 0.8μL pH 3-10 ampholytes, 0.75 μL 2 M DTT and brought up to 150μL with Zoom 2D protein solubilizer 1. 150μL of sample is loaded into IPG runner, and pH 3-10NL IPG strips are added. Strips are soaked overnight at room temperature. A step protocol is used for isoelectric focusing (250V, 20min.; 450V 15min; 750 V 15 min 2000V 30 minutes). For the second dimension, strips are treated for 15 minutes in 1X loading buffer, followed by 15 minutes in 1X loading buffer plus 160 mM iodoacetatic acid. Strips are electrophoresed on NuPAGE 4-12% Bis Tris ZOOM gels. Proteins are blotted onto PVDF 4.5μm membranes. Serines 232, 293 and 300 are targets of the three well-characterized PDK phosphorylation events controlling E1 activity. Equal amounts of protein from treated and mock-treated cells are loaded on gels and western transfers are probed with anti-E1α Ab as an internal matching control or one of the three anti-phospho-E1α Abs.

Animal Study: [1]

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.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, , 30 mg/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.
1

References

[1] Zachar Z, et al. J Mol Med (Berl). 2011, 89(11), 1137-1148.

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01839981 Recruiting Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) 2013-07 Phase 1
NCT01902381 Recruiting Previously Treated Myelodysplastic Syndromes Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) 2013-08
NCT01931787 Recruiting Recurrent Small Cell Lung Cancer Comprehensive Cancer Center of Wake Forest University|National Cancer Institute (NCI) 2013-10
NCT01830322 Withdrawn Metastatic Pancreatic Adenocarcinoma Cornerstone Pharmaceuticals, Inc. 2014-01 Phase 2
NCT01520805 Not yet recruiting Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Cornerstone Pharmaceuticals, Inc. 2015-01 Phase 2

Chemical Information

Download CPI-613 SDF
Molecular Weight (MW) 388.59
Formula

C22H28O2S2

CAS No. 95809-78-2
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 78 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 78 mg/mL (200 mM)
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 Name 6,8-bis(benzylthio)octanoic acid

Research Area

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