CAS: 1246560-33-7; 5-(9-Isopropyl-8-Methyl-2-Morpholino-9H-Purin-6-yl)Pyrimidin-2-Amine
该化合物是一个小分子抑制器,主要以其在定位诱导信号路径方面的作用而闻名.这种复合物具有选择性抑制器的典型特征,表明在肿瘤病和其他与受虐调节的微生物活动有关的疾病中可能存在治疗性应用.VS-5584经常研究其抑制对细胞生长,扩散和生存至关重要的MTORC1和MTORC2复合体的能力.该化合物的特点是其中溶性,在有机溶剂中和水中的溶性相对较低,这是许多小分子抑制剂常见的常见现象.其化学结构包括特定功能组,有助于其结合的亲和感.研究表明,VS-5584可能会提高其他抗癌剂的功效,使其成为组合疗法研究的一个对象.与许多调查性化合物一样,正在进行的研究对于充分阐明其药理学,药用动力学和临床环境中的潜在影响至关重要.
- 英文名称5-(9-Isopropyl-8-Methyl-2-Morpholino-9H-Purin-6-yl)Pyrimidin-2-Amine
- 中文名称5-[8-甲基-9-异丙基-2-(4-吗啉基)-9H-嘌呤-6-基]-2-嘧啶胺
- IUPAC名称5-(9-isopropyl-8-methyl-2-morpholino-9H-purin-6-yl)pyrimidin-2-amine
- CAS编号1246560-33-7
- MFCD编号:MFCD25372027
- FDA UNII编号:W71J4X250V
- 分子式:C17H22N8O分子量:354.42
- 产品CID: 357460
- 同类组份化合物CAS1246535-95-4 (VS-5584 analog)1246560-33-7 (VS-5584)
- 产品分类生物化工 → 抑制剂 → PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR)
物理性质
上下游产品
5-(8-bromo-9-isopropyl-2-morpholin-4-yl-9H-purin-6-yl)-pyrimidin-2-ylamine dimethyl zinc(II)合成工艺路线路线简述
- 合成目标产物 Vs-5584 主要起始原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy- And Dimethylzinc
- (文献来源)合成步骤主要原料 Ethanamine, N-[(3,5-Dichlorophenyl)Methylene]-2,2-Diethoxy- 和 Dimethylzinc
📜5-(8-Bromo-9-Isopropyl-2-Morpholin-4-Yl-9H-Purin-6-yl)-Pyrimidin-2-Ylamine 以47的收率获得5-[8-甲基-9-异丙基-2-(4-吗啉基)-9H-嘌呤-6-基]-2-嘧啶胺
参考文献:Pyrimidine Substituted Purine Compounds As Kinase (S) Inhibitors
标题:Pyrimidine Substituted Purine Compounds As Kinase (S) Inhibitors
摘要:本发明涉及一种能作为激酶抑制剂的嘌呤化合物.该化合物具有以下结构:或其药学上可接受的盐.
海关参考信息
- 2909110000-乙醚
2922110001-单乙醇胺
2921199090-其他无环单胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
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: Chen Y, Tsai HW, Tsai YH, Tseng SH. VS-5584, a PI3K/mTOR dual inhibitor, exerts antitumor effects on neuroblastomas in vitro and in vivo. J Pediatr Surg. 2021 Aug;56(8):1441-1448. doi: 10.1016/j.jpedsurg.2020.10.033. Epub 2020 Nov 5. 20(8):616-623. doi: 10.2174/1568009620666200414150353.
957:176004. doi: 10.1016/j.ejphar.2023.176004. Epub 2023 Aug 23. 75(2):446-55. doi: 10.1158/0008-5472.CAN-14-1223. Epub 2014 Nov 28. 12(2):151-61. doi: 10.1158/1535-7163.MCT-12-0466. Epub 2012 Dec 27.
6: Shao Z, Bao Q, Jiang F, Qian H, Fang Q, Hu X. VS-5584, a Novel PI3K-mTOR Dual Inhibitor, Inhibits Melanoma Cell Growth In Vitro and In Vivo. PLoS One. 2015 Jul 23;10(7):e0132655. doi: 10.1371/journal.pone.0132655.
合成参考文献
参考文献:10.1158/1535-7163.mct-12-0466
摘要:Hart S, Novotny-Diermayr V, Goh KC, Williams M, Tan YC, Ong LC, Cheong A, Ng BK, Amalini C, Madan B, Nagaraj H, Jayaraman R, Pasha KM, Ethirajulu K, Chng WJ, Mustafa N, Goh BC, Benes C, McDermott U, Garnett M, Dymock B, Wood JM. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151–61.
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