CAS: 1082949-68-5; 4-(4-(4-(4-Fluoro-3-(Trifluoromethyl)Phenyl)-1-Methyl-1H-Imidazol-2-yl)Piperidin-1-yl)-1H-Pyrazolo[3,4-D]Pyrimidine 4-Methylbenzenesulfonate
- 英文名称4-(4-(4-(4-Fluoro-3-(Trifluoromethyl)Phenyl)-1-Methyl-1H-Imidazol-2-yl)Piperidin-1-yl)-1H-Pyrazolo[3,4-D]Pyrimidine 4-Methylbenzenesulfonate
- 中文名称LY-2584702对甲苯磺酸盐
- IUPAC名称4-(4-(4-(4-fluoro-3-(trifluoromethyl)phenyl)-1-methyl-1H-imidazol-2-yl)piperidin-1-yl)-1H-pyrazolo[3,4-d]pyrimidine 4-methylbenzenesulfonate
- 其它别名4-[4-[4-[4-Fluoro-3-(Trifluoromethyl)Phenyl]-1-Methyl-1H-Imidazol-2-Yl]-1-Piperidinyl]-1H-Pyrazolo[3,4-D]Pyrimidine 4-Methylbenzenesulfonate (1:1); 4-{4-[4-(4-Fluoro-3-Trifluoromethyl-Phenyl)-1-Methyl-1H-Imidazol-2-Yl]-Piperidin-1-Yl}-1H-Pyrazolo[3,4-D]Pyrimidine P-Toluenesulfonate; Lys6K2; Lys6K2
- CAS编号1082949-68-5
- MFCD编号:MFCD29054739
- 分子式:C28H27F4N7O3S分子量:617.63
- 产品CID: 119672
- 同类组份化合物CAS1082949-68-5 (tosylate)1082949-67-4 (free base)
- 产品分类生物化工 → 抑制剂 → PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR)
物理性质
- PSA:138.27
- LogP:6.6828
- 溶解性DMSO:12.55(Max Conc. mg/mL);20.31(Max Conc. Mm)
- 外观形态淡黄色至黄色结晶性固体
- 储存条件储存在 -20°C
- 产品应用该化合物是P70S6K(IC50=4 NM)的选择性,ATP-竞争抑制剂,在临床前型模型中表现出抗脉冲效果;它抑制HCT116结肠癌细胞中S6核子蛋白质(PS6)(IC50 = 0.1-0.24 ΜM);它与EGFR抑制剂ERLOTINIB或MTOR抑制剂气旋结合时,具有重大的协同效应;它显示在U87MG血压瘤和HCT115结肠皮癌蛋白模型12.5毫克/千克BID中存在重大的抗脉搏活动;它进入了第一阶段临床试验.
上下游产品
4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazol[3,4-d]pyrimidine toluene-4-sulfonic acid合成工艺路线路线简述
📜P70S6K信号转导抑制剂(Ly-2584702Freebase) 以86的收率获得ly-2584702 对甲苯磺酸盐
参考文献:Wo2008140947A1
标题:Wo2008140947A1
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Leohr JK, Luffer-Atlas D, Luo MJ, DeBrota DJ, Green C, Mabry TE, Suico JG. Serum Lipid and Protein Changes in Healthy Dyslipidemic Subjects Given a Selective Inhibitor of p70 S6 Kinase-1. J Clin Pharmacol. 2018 Apr;58(4):412-424. doi: 10.1002/jcph.1032. Epub 2017 Nov 26. doi: 10.1002/jcb.26272. Epub 2017 Aug 28. doi: 10.1371/journal.pone.0182891. eCollection 2017.
4: Estridge TB, Dey AB, Reidy C, Yu X, Zhang Y, Hartley M, Milligan PL, Jin N, Kowala MC, Leohr JK, Fretland AJ, Mabry TE, Luffer-Atlas D, Luo MJ. Identification of 4-Aminopyrazolopyrimidine Metabolite That May Contribute to the Hypolipidemic Effects of LY2584702 in Long Evans Diet-Induced Obese Rats. J Pharmacol Exp Ther. 2017 Jul;362(1):108-118. doi: 10.1124/jpet.117.240242. Epub 2017 May 2. doi: 10.1371/journal.pone.0169804. eCollection 2017.
6: Hollebecque A, Houédé N, Cohen EE, Massard C, Italiano A, Westwood P, Bumgardner W, Miller J, Brail LH, Benhadji KA, Soria JC. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. Eur J Cancer. 2014 Mar;50(5):876-84. doi: 10.1016/j.ejca.2013.12.006. Epub 2014 Jan 20. doi: 10.1016/j.ejca.2013.11.039. Epub 2014 Jan 15.
📝 需求与反馈
尽可能描述清楚需求与问题信息
