CAS: 1225037-39-7; 5-(4,6-Dimorpholino-1,3,5-Triazin-2-yl)-4-(Trifluoromethyl)Pyridin-2-Amine
- 英文名称5-(4,6-Dimorpholino-1,3,5-Triazin-2-yl)-4-(Trifluoromethyl)Pyridin-2-Amine
- 中文名称PI3K/MTOR抑制剂
- IUPAC名称5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine
- CAS编号1225037-39-7
- MFCD编号:MFCD28902193
- FDA UNII编号:6Z3QHB00LB
- 分子式:C17H20F3N7O2分子量:411.39
- 产品CID: 321954
- 同类组份化合物CAS1225037-39-7 (free base)1820902-72-4 (HCl)1820902-73-5 (HCl hydrate)
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 沸点643.7±65.0 °C(预测)
- 密度1.418±0.06 g/cm3(预测)
- pKa:4.92±0.10(预测)
- 溶解性DMSO:22.0(Max Conc. mg/mL);53.48(Max Conc. Mm) DMF:10.0(Max Conc. mg/mL);24.31(Max Conc. Mm) Ethanol:2.0(Max Conc. mg/mL);4.86(Max Conc. Mm)
- 外观形态白色至灰色结晶性固体
- 储存条件储存在 -20°C
- 产品应用该化合物是一种新型脑膜膜双膜PI3K/MTOR抑制剂,在体外和体外有抗淋巴瘤活动;它通过诱导G1细胞循环扣压,在淋巴马细胞大块板(包括DLBCL,MCL,CLL和SMZL)中,特别在B细胞淋巴虫细胞(包括DIBL,ML,CCL,CPL和 SMZ L)中表现出强大的抗生素效应;它抑制了淋巴细胞中的PI-3K/MORTOR信号路径;它作为单一剂或组合疗法中表现出抗淋卜瘤的功效;它显示了PC3前列腺细胞和大鼠PC3色素模型中的抗瘤活动.
MSDS等安全信息
合成工艺路线路线简述
📜(E)-N'-(5-(4,6-Dimorpholino-1,3,5-Triazin-2-yl)-4-(Trifluoromethyl)Pyridin-2-yl)-N,N-Dimethylformimidamide置于盐酸体系中,用 1,4-二氧六环,甲醇 用作溶剂,化学反应 4.0H,以72%的收率获得没货
参考文献: Novel Manufacturing Process For Triazine,Pyrimidine And Pyridine Derivatives[fr] Nouveau Procédé De Fabrication De Dérivés De Triazine,Pyrimidine Et Pyridine
标题: Novel Manufacturing Process For Triazine,Pyrimidine And Pyridine Derivatives[fr] Nouveau Procédé De Fabrication De Dérivés De Triazine,Pyrimidine Et Pyridine
摘要:该发明涉及一种制造三嗪,嘧啶和吡啶衍生物的方法,其化学式为(I),其中u,V,W和z为氮或碳原子,其中至少一个为氮,其他取代基如说明书中所定义,通过将相应的卤代三嗪,嘧啶或吡啶与吡啶基或嘧啶基硼烷进行铂铃偶联反应,其中氨基功能以甲酰胺基进行保护.该发明还涉及适当的中间体和制造这些中间体的方法.此外,该发明还涉及固态纯的5-(4,6-二吗啉基-1,3,5-三嗪-2-基)-4-(三氟甲基)吡啶-2-胺.
海关参考信息
- 2909110000-乙醚
2922110001-单乙醇胺
2933310010-吡啶
2903399090-其他无环烃卤化衍生物 - 💡 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
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: Wind SS, Jansen MAA, Rijsbergen M, van Esdonk MJ, Ziagkos D, Cheng WC, Niemeyer-van der Kolk T, Korsten J, Gruszka A, Schmitz-Rohmer D, Bonnel D, Legouffe R, Barré F, Bekkenk MW, de Haas ERM, Quint KD, Rolli M, Streefkerk HJ, Burggraaf J, Vermeer MH, Rissmann R. Topical Bimiralisib Shows Meaningful Cutaneous Drug Levels in Healthy Volunteers and Mycosis Fungoides Patients but No Clinical Activity in a First-in-Human, Randomized Controlled Trial. Cancers (Basel). 2022 Mar 15;14(6):1510. doi: 10.3390/cancers14061510. Erratum in: Cancers (Basel). 2023 Feb 27;15(5):
2: Johnson FM, Janku F, Gouda MA, Tran HT, Kawedia JD, Schmitz D, Streefkerk H, Lee JJ, Andersen CR, Deng D, Rawal S, Shah PA, El-Naggar AK, Johnson JM, Frederick MJ. Inhibition of the Phosphatidylinositol-3 Kinase Pathway Using Bimiralisib in Loss-of-Function NOTCH1-Mutant Head and Neck Cancer. Oncologist. 2022 Dec 9;27(12):1004-e926. doi: 10.1093/oncolo/oyac185.
3: Seipel K, Brügger Y, Mandhair H, Bacher U, Pabst T. Rationale for Combining the BCL2 Inhibitor Venetoclax with the PI3K Inhibitor Bimiralisib in the Treatment of IDH2- and FLT3-Mutated Acute Myeloid Leukemia. Int J Mol Sci. 2022 Oct 20;23(20):12587. doi: 10.3390/ijms232012587.
合成参考文献
参考文献:10.1021/acs.jmedchem.9b00525
摘要:Rageot D, Bohnacker T, Keles E, McPhail JA, Hoffmann RM, Melone A, Borsari C, Sriramaratnam R, Sele AM, Beaufils F, Hebeisen P, Fabbro D, Hillmann P, Burke JE, Wymann MP. (S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase. J Med Chem. 2019 Jul 11;62(13):6241–61. doi: 10.1021/acs.jmedchem.9b00525.
📝 需求与反馈
尽可能描述清楚需求与问题信息
