|6,8-双(苄基硫基)辛酸|CsnPharm

CAS No.: 95809-78-2

Devimistat/6,8-双(苄硫基)辛酸 Catalog No. CSN15809

Synonyms: CPI-613;6,8-Bis(benzylthio)octanoic acid

CPI-613 is an E1α pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. CPI-613 has been granted orphan drug status by the US FDA for pancreatic cancer.

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实验方案

技术信息

生物活性

描述CPI-613 is a novel anti-tumor compound targeting on PDH. CPI-613 at concentration of 240μM disrupted H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity, and caused loss of mitochondrial membrane potential. It induced extensive post-translational modification of PDH E1 at 300μM, which is acquired high PDK levels. CPI-613 demonstrated anticancer activity both in vitro and in vivo. It induced both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells at concentration of 240μM in 22 or 24h. It showed strong antitumor activity against human non-small cell lung and pancreatic cancers in xenograft models at dose of 25mg/kg^[4]. CPI-613 undergoes both phase 1 (oxidation) and phase 2 (glucuronidation) transformations^[5]. Inhibition of KGDH by CPI-613 may partially contribute to antitumor activity of CPI-613. It inhibited KGDH function strongly and rapidly, selectively in tumor cells. Moreover, CPI-613 induced a correspondingly rapid, powerful redox signal in tumor cell mitochondria^[6].
动物研究
剂量
Mice: 25 mg/kg^[4] (i.p.), 100 mg/kg^[1] (i.p., MTD)

给药途径
i.p.
临床研究

动物研究
剂量	Mice: 25 mg/kg^[4] (i.p.), 100 mg/kg^[1] (i.p., MTD)
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02472626	Untreated Adult Acute Myeloid ... more >>Leukemia Collapse <<	Phase 1 Phase 2	Withdrawn(Drug Supply Issues)	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT02484391	Granulocytic Sarcoma ... more >> Recurrent Adult Acute Myeloid Leukemia Collapse <<	Phase 2	Recruiting	February 2022	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Scarlett Hutchens 336-713-6915 snhutche@wakehealth.edu Principal Investigator: Timothy S. Pardee Collapse <<
NCT01835041	Acinar Cell Adenocarcinoma of ... more >>the Pancreas Duct Cell Adenocarcinoma of the Pancreas Recurrent Pancreatic Cancer Stage IV Pancreatic Cancer Collapse <<	Phase 1	Active, not recruiting	January 2019	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5734 mL
- 12.8671 mL
- 25.7343 mL
- 5 mM
- 0.5147 mL
- 2.5734 mL
- 5.1469 mL
- 10 mM
- 0.2573 mL
- 1.2867 mL
- 2.5734 mL

技术信息

CAS号

95809-78-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H28O2S2

运输

蓝冰

分子量

388.59

别名

CPI-613;6,8-Bis(benzylthio)octanoic acid

溶解度

DMSO	150.0 mg/mL (386.0 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02472626	Untreated Adult Acute Myeloid ... more >>Leukemia Collapse <<	Phase 1 Phase 2	Withdrawn(Drug Supply Issues)	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT02484391	Granulocytic Sarcoma ... more >> Recurrent Adult Acute Myeloid Leukemia Collapse <<	Phase 2	Recruiting	February 2022	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Scarlett Hutchens 336-713-6915 snhutche@wakehealth.edu Principal Investigator: Timothy S. Pardee Collapse <<
NCT01835041	Acinar Cell Adenocarcinoma of ... more >>the Pancreas Duct Cell Adenocarcinoma of the Pancreas Recurrent Pancreatic Cancer Stage IV Pancreatic Cancer Collapse <<	Phase 1	Active, not recruiting	January 2019	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT01766219	Adult Primary Cholangiocellula... more >>r Carcinoma Advanced Adult Primary Liver Cancer Cholangiocarcinoma of the Extrahepatic Bile Duct Cholangiocarcinoma of the Gallbladder Localized Unresectable Adult Primary Liver Cancer Metastatic Extrahepatic Bile Duct Cancer Recurrent Adult Primary Liver Cancer Recurrent Extrahepatic Bile Duct Cancer Unresectable Extrahepatic Bile Duct Cancer Collapse <<	Phase 1 Phase 2	Completed	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT01839981	Acinar Cell Adenocarcinoma of ... more >>the Pancreas Duct Cell Adenocarcinoma of the Pancreas Recurrent Pancreatic Cancer Stage III Pancreatic Cancer Stage IV Pancreatic Cancer Collapse <<	Phase 1	Completed	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT02232152	Mucinous Adenocarcinoma of the... more >> 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 Collapse <<	Phase 1	Recruiting	December 2018	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Stefan Grant, MD 336-713-5172 scgrant@wakehealth.edu Principal Investigator: Stefan Grant Collapse <<
NCT01902381	Previously Treated Myelodyspla... more >>stic Syndromes Collapse <<	Phase 2	Suspended(Lack of accrual)	December 2018	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT02168140	Adult Lymphocyte Depletion Hod... more >>gkin Lymphoma Adult Lymphocyte Predominant Hodgkin Lymphoma Adult Mixed Cellularity Hodgkin Lymphoma Adult Nasal Type Extranodal NK/T-cell Lymphoma Adult Nodular Sclerosis Hodgkin Lymphoma Anaplastic Large Cell Lymphoma Angioimmunoblastic T-cell Lymphoma Hepatosplenic T-cell Lymphoma Noncutaneous Extranodal Lymphoma Peripheral T-cell Lymphoma Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Hodgkin Lymphoma Recurrent Adult T-cell Leukemia/Lymphoma Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma Recurrent Mycosis Fungoides/Sezary Syndrome T-cell Adult Acute Lymphoblastic Leukemia T-cell Large Granular Lymphocyte Leukemia Collapse <<	Phase 1	Recruiting	July 2020	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Recruiting Winston-Salem, North Carolina, United States, 27157 Contact: Zanetta S. Lamar 336-716-7448 zlamar@wakehealth.edu Principal Investigator: Zanetta S. Lamar United States, Pennsylvania Abramson Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19104 Contact: Joseph Vena, RN mailto:Joseph.Vena@uphs.upenn.edu Contact: Tanya Latorre mailto:Tanya.Latorre@uphs.upenn.edu Collapse <<
NCT00907166	Cancer Pancre... more >>atic Cancer Pancreatic Carcinoma Collapse <<	Phase 1 Phase 2	Terminated(Suspended trial was... more >> not restarted.) Collapse <<	December 2017	United States, New York ... more >> Eastchester Center for Cancer Care Bronx, New York, United States, 10469 United States, Texas Mary Crowley Cancer Research Centers Dallas, Texas, United States, 75201 Collapse <<
NCT03504423	Pancreatic Cancer Metastatic	Phase 3	Recruiting	March 2022	United States, North Carolina ... more >> Wake Forest Baptist Health Recruiting Winston-Salem, North Carolina, United States, 27157 Principal Investigator: Caio Max Rocha Lima, MD Collapse <<
NCT02168907	B-cell Adult Acute Lymphoblast... more >>ic 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 Collapse <<	Phase 1	Terminated(Slow Accruals)	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT01830322	Metastatic Pancreatic Adenocar... more >>cinoma Collapse <<	Phase 2	Withdrawn	December 2018	United States, New York ... more >> Eastchester Center for Cancer Care Bronx, New York, United States, 10469 United States, Texas Temple Vasicek Cancer Treatment Center Temple, Texas, United States, 76508 Collapse <<
NCT01034475	Advanced Hematologic Malignanc... more >>ies Collapse <<	Phase 1	Completed	-	United States, North Carolina ... more >> Wake Forest University Health Sciences Winston-Salem, North Carolina, United States, 27012 Collapse <<
NCT01768897	Adult Acute Myeloid Leukemia W... more >>ith 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 Collapse <<	Phase 1	Completed	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT00741403	Advanced Cancer ... more >> Metastatic Cancer Lymphoma Solid Tumors Advanced Malignancies Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Pivotal Research Centers Peoria, Arizona, United States, 85381 United States, New York Eastchester Center for Cancer Care Bronx, New York, United States, 10469 United States, Texas Mary Crowley Cancer Research Centers Dallas, Texas, United States, 75201 Canada, British Columbia British Columbia Cancer Agency Vancouver, British Columbia, Canada Collapse <<
NCT01520805	Acute Myeloid Leukemia (AML) ... more >> Myelodysplastic Syndrome (MDS) Collapse <<	Phase 2	Withdrawn	December 2018	United States, New Jersey ... more >> Cornerstone Pharmaceuticals, Inc Cranbury, New Jersey, United States, 08512 Collapse <<
NCT01931787	Recurrent Small Cell Lung Canc... more >>er Collapse <<	Phase 1	Completed	-	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT03504410	Relapsed/Refractory Acute Myel... more >>oid Leukemia Collapse <<	Phase 3	Recruiting	March 2023	United States, North Carolina ... more >> Wake Forest Baptist Health Recruiting Winston-Salem, North Carolina, United States, 27157 Principal Investigator: Bayard L Powell, MD United States, Ohio Cleveland Clinic Recruiting Cleveland, Ohio, United States, 44195 Principal Investigator: Aziz Nazha, MD Collapse <<
NCT03374852	Pancreatic Ductal Adenocarcino... more >>ma Collapse <<	Phase 2	Withdrawn(PI Left institution ... more >>on 8/6/2018 and study has been final reported with IRB. Never opened to accrual) Collapse <<	October 2020	-
NCT03370159	Stage IIIB Non-Small Cell Lung... more >> Cancer AJCC v7 Stage IV Non-Small Cell Lung Cancer AJCC v7 Collapse <<	Phase 1 Phase 2	Withdrawn(Sponsor decided not ... more >>to move forward) Collapse <<	March 1, 2020	United States, North Carolina ... more >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 Collapse <<
NCT03435289	Pancreatic Cancer ... more >> Metastatic Pancreatic Cancer Collapse <<	Phase 1	Recruiting	January 2019	United States, New Jersey ... more >> Morristown Medical Center Recruiting Morristown, New Jersey, United States, 07960 Contact: Nancy Ginder, BSN, OCN 973-971-6608 nancy.ginder@atlantichealth.org Sub-Investigator: Joshua Strauss, MD Principal Investigator: Angela T Alistar, MD Overlook Medical Center Recruiting Summit, New Jersey, United States, 07901 Contact: Christopher Buck, BSN, MS 908-522-2043 christopher.buck@atlantichealth.org Sub-Investigator: Sophie D Morse, MD Collapse <<
NCT03699319	Pancreatic Cancer	Phase 2	Recruiting	January 1, 2021	United States, Ohio ... more >> University Hospitals Seidman Cancer Center, Case Comprehensive Cancer Center Recruiting Cleveland, Ohio, United States, 44106 Contact: Jeffrey Hardacre, MD 800-641-2422 cancer@case.edu Collapse <<
NCT01832857	Cancer	Phase 2	Terminated	-	United States, New York ... more >> Eastchester Center for Cancer Care Bronx, New York, United States, 10469 Collapse <<

Devimistat/6,8-双(苄硫基)辛酸 Catalog No. CSN15809

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