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| | RIOK2-IN-1 Basic information |
| | RIOK2-IN-1 Chemical Properties |
| Boiling point | 540.741±38.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.218±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 10.494±0.46(predicted) |
| | RIOK2-IN-1 Usage And Synthesis |
| Uses | RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression[1]. | | References | [1] Ouyang Y, et al. Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. J Med Chem. 2022 Jun 9;65(11):7833-7842. DOI:10.1021/acs.jmedchem.2c00271 |
| | RIOK2-IN-1 Preparation Products And Raw materials |
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