CAS: 1255517-76-0; 2-((4-(5-Ethylpyrimidin-4-yl)Piperazin-1-yl)Methyl)-6-(Trifluoromethyl)-1H-Benzo[d]Imidazole

上下游产品

5-ethyl-4-(piperazin-1-yl)pyrimidine 2-(chloromethyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole 5-ethyl-pyrimidin-4-ol

📜5-乙基-4(1H)-嘧啶酮置于benzotriazol-1-Yloxyl-Tris-(Pyrrolidino)-Phosphonium Hexafluorophosphate,1,8-二氮杂双环[5.4.0]十一碳-7-烯,N,N-二异丙基乙胺,三氟乙酸体系中,用 二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 69.5H,反应生成2-[[4-(5-乙基-4-嘧啶基)-1-哌嗪基]甲基]-6-(三氟甲基)-1H-苯并咪唑
参考文献:Characterization Of Pf-4708671,A Novel And Highly Specific Inhibitor Of P70 Ribosomal S6 Kinase (S6K1)
标题:Characterization Of Pf-4708671,A Novel And Highly Specific Inhibitor Of P70 Ribosomal S6 Kinase (S6K1)
摘要:S6K1(p70 核糖体 S6 激酶 1)通过 Pi3K(磷脂酰肌醇 3-激酶)和 Mtor(哺乳动物雷帕霉素靶标)信号通路被胰岛素和生长因子激活.S6K1 调节蛋白质合成,生长,增殖和长寿等多个过程,抑制 S6K1 已被提出作为治疗癌症和胰岛素抵抗的一种策略.本文介绍了一种新型细胞渗透性 S6K1 抑制剂 Pf-4708671,它能特异性抑制 S6K1 异构体,Ki 为 20 Nm,Ic50 为 160 Nm.Pf-4708671 能阻止 S6K1 介导的 S6 蛋白对 Igf-1(胰岛素样生长因子 1)的磷酸化反应,同时对 Pma 诱导的高度相关的 Rsk(p90 核糖体 S6 激酶)和 Msk(丝裂原和应激激活激酶)激酶底物的磷酸化没有影响.研究还发现,Pf-4708671 能诱导 S6K1 的 T 环和疏水基团发生磷酸化,这种作用依赖于 Mtorc1(mtor 复合物 1).Pf-4708671 是首个报道的 S6K1 特异性抑制剂,将成为界定 S6K1置于mtor 下游特异性作用的有用工具.
Doi:10.1042/bj20101024

专利信息

专利号:US-11801232-B2
优先权日:2019-11-27
标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
发明人：HUANG GLORIA
权利人:UNIV YALE
摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.