CPI-613

SKU: orb1301026

Description

Devimistat is a lipoate analog that disrupts cancer cell metabolism by inhibiting the mitochondrial enzymes pyruvate dehydrogenase and α-ketoglutarate dehydrogenase. Its antineoplastic potential has been investigated in preclinical studies and clinical trials for various solid tumors, including pancreatic cancer and lymphoma.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 95809-78-2
• MW: 388.59
• Purity: >98%
• Formula: C₂₂H₂₈O₂S₂
• SMILES: OC(=O)CCCCC(CCSCc1ccccc1)SCc1ccccc1
• Target: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH)
• Solubility: Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml)

Bioactivity

• In Vivo:
  Devimistat (25 mg/kg) has potent anticancer activity in a human tumor xenograft model of of a pancreatic tumor cell (BxPC-3). Similarly, Devimistat (10 mg/kg) also produces significant tumor growth inhibition of H460 human non-small cell lung carcinoma in mouse model. Besides, Devimistat 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.
• In Vitro:
  In vitro, Devimistat 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. Devimistat 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, Devimistat (240 μM) also induces both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Devimistat

Compound Identifiers

PubChem CID

24770514