CPI-613是一种Lipoate类似物，在NCI-H460 细胞系中抑制线粒体酶pyruvate dehydrogenase (PDH)和α-ketoglutarate dehydrogenase，干扰肿瘤细胞线粒体代谢。

98% min

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

CPI 613; CPI613

DMSO 78 mg/mL warmed (200.72 mM)

Ethanol 78 mg/mL (200.72 mM)

Water Insoluble

PDH ,α-ketoglutarate dehydrogenase

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.

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