CPI-613 is an E1α pyruvatedehydrogenase (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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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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].
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