2017年12月3日星期日

COH29 |cas 1190932-38-7

COH29 |cas 1190932-38-7

DC Chemicals, Website: www.dcchemicals.com

Product Name: COH29|Cas Number: 1190932-38-7| Catalog Number: DC10430|Other Nmaes: COH-29; COH 29

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity with an IC50 of 8 μM in KB cell.

COH29 overcome hydroxyurea and gemcitabine resistance in cancer cells. It effectively inhibits proliferation of most cell lines in the NCI 60 human cancer panel, most notably ovarian cancer and leukemia, but exerts little effect on normal fibroblasts or endothelial cells. Site-directed mutagenesis, NMR and surface plasmon resonance biosensor studies confirm COH29 binding to the proposed ligand-binding pocket and offer evidence for assembly blockade of the RRM1-RRM2 quaternary structure[1].COH29 results in a dose-dependent inhibition of MOLT-4 tumor xenograft growth with twice-daily oral dosing at 50 mg/kg and 100 mg/kg, which is pronounced by Day 12 of treatment. Similarly, 7 days of treatment of mice bearing TOV11D xenografts with 200, 300, or 400 mg/kg/day COH29 results in a dose-dependent inhibition of tumor xenograft growth. Tumor growth is significantly inhibited compared with the control group[1].

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