| 產(chǎn)品描述： | 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. |
| 靶點(diǎn)： |
IC50: 8 μM (RNR, KB cell), 31.57±3.35 μM (RNR, OV90 cell);DNA/RNASynthesis |
| 體外研究： |
COH29 (RNR Inhibitor 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 |
| 體內(nèi)研究： |
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 |
| 參考文獻(xiàn)： |
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. 2. Chen MC, et al. The Novel Ribonucleotide Reductase Inhibitor COH29 Inhibits DNA Repair In Vitro. Mol Pharmacol. 2015 Jun;87(6):996-1005. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.378 ml |
11.892 ml |
23.785 ml |
| 5 mM |
0.476 ml |
2.378 ml |
4.757 ml |
| 10 mM |
0.238 ml |
1.189 ml |
2.378 ml |
| 50 mM |
0.048 ml |
0.238 ml |
0.476 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
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危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲(chǔ)）
營業(yè)執(zhí)照(三證合一)
北京