中文名 | UNC 0631 |
英文名 | UNC 0631 |
别名 | 化合物UNC0631 G9A抑制剂(UNC 0631) N-[1-(环己基甲基)-4-哌啶基]-2-[六氢-4-异丙基-1H-1,4-二氮杂卓-1-基]-6-甲氧基-7-[3-(1-哌啶基)丙氧基]-4-喹唑啉胺 |
英文别名 | CS-793 UNC 0631 N-[1-(Cyclohexylmethyl)-4-piperidinyl]-2-(4-isopropyl-1,4-diazepa n-1-yl)-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine N-(1-(cyclohexylmethyl)piperidin-4- yl)-2-(4-isopropyl-1,4-diazepan-1-yl)- 6-methoxy-7-(3-(piperidin-1- yl)propoxy)quinazolin-4-amine N-[1-(CyclohexylMethyl)-4-piperidinyl]-2-[hexahydro-4-(1-Methylethyl)-1H-1,4-diazepin-1-yl]-6-Methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinaMine N-[1-(Cyclohexylmethyl)-4-piperidinyl]-2-[hexahydro-4-(1-methylethyl)-1H-1,4-diazepin-1-yl]-6-methoxy-7-[3-(1-piperidinyl)propoxy]-4-quinazolinamine UNC0631 |
CAS | 1320288-19-4 |
EINECS | 604-604-1 |
化学式 | C37H61N7O2 |
分子量 | 635.93 |
密度 | 1.114±0.06 g/cm3(Predicted) |
沸点 | 763.4±70.0 °C(Predicted) |
溶解度 | 溶于DMSO,不溶于水 |
酸度系数 | 9.34±0.70(Predicted) |
存储条件 | 2-8 ℃, dark |
靶点 | G9a |
体外研究 | UNC 0631 (Compound 7) has high cellular potency and excellent separation of functional potency versus cell toxicity in a variety of cell lines. UNC 0631 is highly potent in reducing H3K9me2 levels and has low cell toxicity. UNC 0631 reduces H3K9me2 levels with ICW IC 50 values of 25 nM, 18 nM, 26 nM, 24 nM, 51 nM, 72 nM and 46 nM in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT 116 p53 -/- and IMR90 cell lines, respectively. |
参考资料 展开查看 | 1: Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. doi: 10.1021/jm200903z. Epub 2011 Aug 5. PubMed PMID: 21780790; PubMed Central PMCID: PMC3171737. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.573 ml | 7.863 ml | 15.725 ml |
5 mM | 0.315 ml | 1.573 ml | 3.145 ml |
10 mM | 0.157 ml | 0.786 ml | 1.573 ml |
5 mM | 0.031 ml | 0.157 ml | 0.315 ml |
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