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Devimistat

Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂，还是一种lipoic acid 拮抗剂，能阻断线粒体能量代谢，诱导多种癌细胞凋亡。

CAS号

95809-78-2

分子式

C22H28O2S2

主要靶点

Apoptosis|Dehydrogenase|Mitochondrial Metabolism

仅限科研使用

Cat No : CM03649

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Synonyms

6,8-Bis(benzylthio)octanoic acid|CPI613|CPI 613|辛酸|CPI-613

验证数据展示

  • CAS No.: 95809-78-2

    Devimistat
    CAS#: 95809-78-2

产品信息

CPI-613, a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others.

CAS号 95809-78-2
分子式 C22H28O2S2
主要靶点 Apoptosis|Dehydrogenase|Mitochondrial Metabolism
主要通路 代谢|凋亡
分子量 388.59
纯度 99.08%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 6,8-Bis(benzylthio)octanoic acid|CPI613|CPI 613|辛酸|CPI-613

体内活性

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]

体外活性

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]

溶解度

DMSO:78 mg/mL (200.72 mM),Ethanol:78 mg/mL (200.72 mM),H2O:<1 mg/mL

参考文献

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

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