COH-29
COH-29 Basic information
- Product Name:
- COH-29
- Synonyms:
-
- COH-29
- N-(4-(3,4-dihydroxyphenyl)-5-phenylthiazol-2-yl)-3,4-dihydroxybenzamide
- 181687
- COH-29; COH 29
- CS-2737
- RNR Inhibitor COH29
- Benzamide, N-[4-(3,4-dihydroxyphenyl)-5-phenyl-2-thiazolyl]-3,4-dihydroxy-
- ribonucleotide,RNR,inhibit,COH-29,reductase,DNA/RNA Synthesis,COH29,RNR Inhibitor COH-29,subunit,COH 29,RNR Inhibitor COH 29,Inhibitor,anticancer
- CAS:
- 1190932-38-7
- MF:
- C22H16N2O5S
- MW:
- 420.44
- Mol File:
- 1190932-38-7.mol
COH-29 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:45.0(Max Conc. mg/mL);107.03(Max Conc. mM)
Ethanol:10.0(Max Conc. mg/mL);23.78(Max Conc. mM) - form
- Solid
- color
- Light yellow to yellow
COH-29 Usage And Synthesis
Uses
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
in vivo
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].
References
[1] Zhou B, et al. A small-molecule blocking ribonucleotide reductase holoenzyme formation inhibits cancer cell growth and overcomes drug resistance.Cancer Res. 2013 Nov 1;73(21):6484-93. DOI:10.1158/0008-5472.CAN-13-1094
[2] Chen MC, et al. The Novel Ribonucleotide Reductase Inhibitor COH29 Inhibits DNA Repair In Vitro. Mol Pharmacol. 2015 Jun;87(6):996-1005. DOI:10.1124/mol.114.094987
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