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CPI-613

CPI-613是Lipoate类似物，抑制线粒体酶pyruvate dehydrogenase (PDH)（丙酮酸脱氢酶）和α-ketoglutarate dehydrogenase（α-酮戊二酸脱氢酶），干扰肿瘤细胞线粒体代谢。

目录号
EY0939
EY0939
EY0939
纯度
99.27%
99.27%
99.27%
规格
1 mg
5 mg
10 mg
原价
280
600
750
售价
280
600
750
库存
现货
现货
现货
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  • 生物活性

    CPI-613 inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase. Disrupts tumor cell mitochondrial metabolism, and increases mitochondrial reactive oxygen species (ROS) production in H460 lung carcinoma cells. Has no effect on KGDH activity in normal bronchial epithelial cells. Induces cell death of multiple tumor cell lines selectively over normal cells in vitro.

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Zachar Z, et al. J Mol Med (Berl). 2011, 89(11), 1137-1148.
    [2] Stuart et al (2014) A strategically designed small molecule attacks alpha-ketoglutarate dehydrogenase in tumor cells through a redox process. Cancer Metab. 2 4.

    分子式
    C22H28O2S2    		 分子量
    388.59    		 CAS号
    95809-78-2    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >50 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    >50 mg/mL

    体内溶解度

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

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00741403 Advanced Cancer|Metastatic Cancer|Lymphoma|Solid Tumors|Advanced Malignancies Drug: CPI-613 Cornerstone Pharmaceuticals, Inc. Phase 1 2008-08-01 2016-12-28
    NCT01520805 Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS) Drug: CPI-613 Cornerstone Pharmaceuticals, Inc. Phase 2 2016-01-01 2016-12-27
    NCT01832857 Cancer Drug: CPI-613 Cornerstone Pharmaceuticals, Inc. Phase 2 2013-06-01 2016-12-27
    NCT01034475 Advanced Hematologic Malignancies Drug: CPI-613 Wake Forest University Health Sciences Phase 1 2010-03-01 2017-01-17
    NCT00907166 Cancer|Pancreatic Cancer|Pancreatic Carcinoma Drug: CPI-613|Drug: CPI-613|Drug: Gemcitabine|Drug: Gemcitabine|Drug: Gemcitabine Cornerstone Pharmaceuticals, Inc. Phase 1|Phase 2 2009-05-01 2017-03-19
    NCT01768897 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 Drug: CPI-613|Drug: cytarabine|Drug: mitoxantrone hydrochloride|Other: laboratory biomarker analysis|Other: pharmacological study Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2013-01-01 2016-12-23
    NCT01931787 Recurrent Small Cell Lung Cancer Drug: 6,8-bis(benzylthio)octanoic acid Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2013-10-01 2016-12-23
    NCT01830322 Metastatic Pancreatic Adenocarcinoma Drug: CPI-613|Drug: Gemcitabine|Drug: Any non-gemcitabine chemotherapies or best supportive care Cornerstone Pharmaceuticals, Inc. Phase 2 2014-01-01 2013-08-13
    NCT02168140 Adult Lymphocyte Depletion Hodgkin 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 Drug: 6,8-bis(benzylthio)octanoic acid|Drug: bendamustine hydrochloride Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2014-09-01 2017-03-13
    NCT01902381 Previously Treated Myelodysplastic Syndromes Drug: 6,8-bis(benzylthio)octanoic acid Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 2 2013-08-01 2017-01-17
    NCT02168907 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|Waldenstr枚m Macroglobulinemia Drug: 6,8-bis(benzylthio)octanoic acid|Drug: bendamustine hydrochloride|Biological: rituximab|Other: laboratory biomarker analysis Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2014-12-01 2017-02-20
    NCT02232152 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 Drug: 6,8-bis(benzylthio)octanoic acid|Drug: fluorouracil|Other: pharmacological study|Other: laboratory biomarker analysis Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2014-12-01 2017-03-13
    NCT01766219 Adult Primary Cholangiocellular 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 Drug: 6,8-bis(benzylthio)octanoic acid Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1|Phase 2 2013-05-01 2017-03-13
    NCT01839981 Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage III Pancreatic Cancer|Stage IV Pancreatic Cancer Drug: 6,8-bis(benzylthio)octanoic acid Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2013-07-01 2017-03-13
    NCT01835041 Acinar Cell Adenocarcinoma of the Pancreas|Duct Cell Adenocarcinoma of the Pancreas|Recurrent Pancreatic Cancer|Stage IV Pancreatic Cancer Drug: 6,8-bis(benzylthio)octanoic acid|Drug: oxaliplatin|Drug: leucovorin calcium|Drug: irinotecan hydrochloride|Drug: fluorouracil|Other: laboratory biomarker analysis Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1 2013-04-01 2017-03-13
    NCT02484391 Granulocytic Sarcoma|Recurrent Adult Acute Myeloid Leukemia Drug: 6,8-Bis(benzylthio)octanoic Acid|Drug: Cytarabine|Procedure: Hematopoietic Cell Transplantation|Drug: Mitoxantrone Hydrochloride Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 2 2015-09-01 2017-02-20
    NCT02472626 Untreated Adult Acute Myeloid Leukemia Drug: 6,8-Bis(benzylthio)octanoic Acid|Drug: Cytarabine|Drug: Daunorubicin Hydrochloride Wake Forest University Health Sciences|National Cancer Institute (NCI) Phase 1|Phase 2 2015-12-01 2017-01-17

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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