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C-02

CAT: 0931-T83889-01Size: 500 µgDry Ice: NoHazardous: No
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CAT#:0931-T83889-01Size:500 µg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Target
Others
Related Pathways
Others
Bioactivity
C-02, a proteolysis-targeting chimera (PROTAC) that combines the hexokinase inhibitor lonidamine with the cereblon ligand thalidomide, effectively induces the degradation of hexokinase 2 in 786-O and PANC-1 cells at a concentration of 20 μM. This compound exhibits cytotoxicity to a range of cancer cells, including 786-O, 4T1, PANC-1, HGC-27, and MCF-7, with IC50 values of 34.07 μM, 5.08 μM, 31.53 μM, 6.11 μM, and 21.65 μM, respectively. Additionally, at 20 μM, C-02 diminishes both the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, suggesting a suppression of glycolysis and mitochondrial damage. In vivo studies reveal that at a dosage of 50 mg/kg, C-02 not only reduces tumor volume but also promotes intratumoral cytokine accumulation and triggers pyroptosis in a 4T1 murine mammary carcinoma model.
Smiles
O=C(N(C1C(NC(CC1)=O)=O)C2=O)C3=C2C=CC=C3NCCCCNC(C4=NN(CC5=C(Cl)C=C(Cl)C=C5)C6=C4C=CC=C6)=O
Molecular Formula
C32H28Cl2N6O5
Molecular Weight
647.51
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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