C-02

Formulation: A solid

Formal Name: 1-(2,4-dichlorobenzyl)-N-(4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butyl)-1H-indazole-3-carboxamide

Purity: ≥95%

Formula Markup: C32H28Cl2N6O5

Formula Weight: 647,5

Shelf life (days): 1095

Notes: C-02 is a proteolysis-targeting chimera (PROTAC) composed of the hexokinase inhibitor lonidamine (Item No. 14640) linked to the cereblon ligand thalidomide (Item No. 14610).{68569} It induces degradation of hexokinase 2 in 786-O and PANC-1 cells when used at a concentration of 20 µM. C-02 is cytotoxic to 786-O, 4T1, PANC-1, HGC-27, and MCF-7 cancer cells (IC50s = 34.07, 5.08, 31.53, 6.11, and 21.65 µM, respectively). It reduces the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, indicating inhibition of glycolysis and mitochondrial damage, respectively, when used at a concentration of 20 µM. In vivo, C-02 (50 mg/kg) reduces tumor volume and induces intratumoral cytokine accumulation and pyroptosis in a 4T1 murine mammary carcinoma model.

• SKU: CAY39384-5
• Manufacturer: Cayman Chemical
• Manufacturer SKU: 39384-5
• Package Unit: 5 mg
• Quantity Unit: STK