CAS: 900185-02-6; 2-((4-Amino-3-(3-Hydroxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Methyl)-5-Methyl-3-(O-Tolyl)Quinazolin-4(3H)-One
该化合物是一种化学化合物,主要作为磷酰胺三基酶(PI3K)路径的选择性抑制器,对各种细胞过程,包括生长,扩散和存活至关重要,该化合物在肿瘤学中的潜在治疗用途特别突出,因为它可能有助于针对显示异常PI3K信号的癌症细胞. PIK-294的特点是它能够选择性地抑制PI3K的特定异形,从而最大限度地减少离目标效果,提高癌症治疗的功效.该化合物通常在药物开发的背景下研究,因为其药效,生物利用率和安全性简介是评估的.与许多实验性化合物一样,有关其溶性,稳定性和再活性的详细信息对于了解其在生物系统中的行为及其作为治疗剂的潜力至关重要.正在进行进一步的研究,以阐明其生物效应和治疗潜力的全部范围.
- 英文名称2-((4-Amino-3-(3-Hydroxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Methyl)-5-Methyl-3-(O-Tolyl)Quinazolin-4(3H)-One
- 中文名称2-[[4-氨基-3-(3-羟基苯基)-1H-吡唑并[3,4-D]嘧啶-1-基]甲基]-5-甲基-3-(2-甲基苯基)-4(3H)-喹唑啉酮
- IUPAC名称2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one
- 其它别名2-{[4-Amino-3-(3-Hydroxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-Yl]Methyl}-5-Methyl-3-(2-Methylphenyl)Quinazolin-4(3H)-One; 4(3H)-Quinazolinone,2-[[4-Amino-3-(3-Hydroxyphenyl)-1H-Pyrazolo[3,4-D]Pyrimidin-
- CAS编号900185-02-6
- MFCD编号:MFCD17019338
- EINECS号:110-148-9
- 分子式:C28H23N7O2分子量:489.54
- 产品CID: 1931044
- 产品分类生物化工 → 抑制剂 → PI3K/Akt/mTOR抑制剂(PI3K/Akt/mTOR)
物理性质
MSDS等安全信息
欧盟法规
C&L通报合成工艺路线路线简述
海关参考信息
- 2902300000-甲苯
2908199090-其他酚的卤化衍生物
2908999090-其他酚的硝化衍生物
2918290000-其他含酚基羧酸 - 💡 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. Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. PCT Int. Appl. (2013), WO 2013147649 A2 20131003 . 2. Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. Jane, Stephen M.; Darido, Charbel. PCT Int. Appl. (2013), WO 2013029116 A1 20130307. 3. Methods for treating oncovirus positive cancers. Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. PCT Int. Appl. (2012), WO 2012118978 A1 20120907. 4. Use of phosphatidylinositol-3'-kinase (PI3K) p110 delta isoform inhibitors for treating retroviral infection and replication. Katsikis, Peter D.; Boesteanu, Alina C.; Turner, Martin. PCT Int. Appl. (2012), WO 2012009452 A1 20120119. 5. Methods and compositions for treatment of ophthalmic conditions. Wilson, Troy Edward; Rommel, Christian; Liu, Yi; Ren, Pingda. PCT Int. Appl. (2010), WO 2010059593 A1 20100527. 6. Discovery of Dual Inhibitors of the Immune Cell PI3Ks p110δ and p110γ: A Prototype for New Anti-inflammatory Drugs. Williams, Olusegun; Houseman, Benjamin T.; Kunkel, Eric J.; Aizenstein, Brian; Hoffman, Randy; Knight, Zachary A.; Shokat, Kevan M. Chemistry & Biology (Cambridge, MA, United States) (2010), 17(2), 123-134. 7. Preparation of pyrazolopyrimidinylmethyl quinazolinones as PI3 kinase antagonists. Knight, Zachary A.; Shokat, Kevan M.; Williams, Olesegun. PCT Int. Appl. (2008), WO 2008127226 A2 20081023. 8.Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Apsel, Beth; Blair, Jimmy A.; Gonzalez, Beatriz; Nazif, Tamim M.; Feldman, Morri E.; Aizenstein, Brian; Hoffman, Randy; Williams, Roger L.; Shokat, Kevan M.; Knight, Zachary A. Nature Chemical Biology (2008), 4(11), 691-699. 9.A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Knight, Zachary A.; Gonzalez, Beatriz; Feldman, Morri E.; Zunder, Eli R.; Goldenberg, David D.; Williams, Olusegun; Loewith, Robbie; Stokoe, David; Balla, Andras; Toth, Balazs; et al. Cell (Cambridge, MA, United States) (2006), 125(4), 733-747.合成参考文献
参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
📝 需求与反馈
尽可能描述清楚需求与问题信息
