CAS: 1448169-71-8; (S)-1-(3-(4-Amino-3-((3,5-Dimethoxyphenyl)Ethynyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Pyrrolidin-1-yl)Prop-2-En-1-One
该化合物是一个具有高度选择性的,不可逆转的抑制纤维状生长因子受体1-4的抑制器,旨在针对与各种癌症有关的受体调节的FGFR信号路径. 它的共价约束机制确保了FGFR活动的持续抑制,为FGFR改变肿瘤提供了潜在效果,包括抗性突变. 临床和临床研究表明它有能力克服可逆FGFR抑制剂所见的共同抗药机制. Futibatinib 展示了有利的药用植物动力特性,包括口服生物利用率和持续的目标接触. 它正在调查与FGFFR畸变的合价性细胞瘤和其他固态肿瘤,强调它作为临床治疗精度的承诺.
- 英文名称(S)-1-(3-(4-Amino-3-((3,5-Dimethoxyphenyl)Ethynyl)-1H-Pyrazolo[3,4-D]Pyrimidin-1-yl)Pyrrolidin-1-yl)Prop-2-En-1-One
- 中文名称1-[(3S)-3-[4-氨基-3-[2-(3,5-二甲氧基苯基)乙炔基]-1H-吡唑并[3,4-d]嘧啶-1-基]-1-吡咯烷基]-2-丙烯-1-酮
- IUPAC名称(S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one
- CAS编号1448169-71-8
- MFCD编号:MFCD29037352
- FDA UNII编号:4B93MGE4AL
- 分子式:C22H22N6O3分子量:418.46
- 产品CID: 683230
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 沸点733.8±60.0 °C(预测)
- 密度1.33±0.1 g/cm3(预测)
- pKa:3.60±0.30(预测)
- 溶解性DMSO:38.0(Max Conc. mg/mL);90.81(Max Conc. Mm) DMF:30.0(Max Conc. mg/mL);71.69(Max Conc. Mm) DMF:Pbs (Ph 7.2) (1:5):0.16(Max Conc. mg/mL);0.38(Max Conc. Mm) Ethanol:0.5(Max Conc. mg/mL);1.19(Max Conc. Mm)
- 外观形态白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TAIHO制药公司和TAITO肿瘤学公司开发的一种口服小分子药物,是纤维生长因子受体1-4的不可逆转的选择性抑制剂. FUTITATIMIB在各种癌症的发育和演变中发挥着关键作用,包括乳腺癌,胆碱酯酶癌,胃癌,非小型细胞肺癌,食道癌和宫颈癌.通过抑制FGFR活动,FUTIBATINIB减少肿瘤细胞扩散和生存.FUTITIBATEINIB在美国获得加速批准,治疗持有FGRFR基因改变的高级固态肿瘤患者.此外,美国还批准对以前治疗过,无法治疗或接受过剖析或受控的内血细胞癌癌患者进行治疗,这些患者在前化学治疗后已经取得进展. FTIBATINI B 的开发和批准为患有FG FRFER突变的癌症患者提供了新的有针对性的治疗选择.
合成工艺路线路线简述
📜3-氯丙酰氯 以85.3%的收率获得1-[(3S)-3-[4-氨基-3-[2-(3,5-二甲氧基苯基)乙炔基]-1H-吡唑并[3,4-D]嘧啶-1-基]-1-吡咯烷基]-2-丙烯-1-酮
参考文献:Method For Producing Dimethoxybenzene Compound
标题:Method For Producing Dimethoxybenzene Compound
摘要:一种生产由化学式(A-1)或其盐表示的化合物的方法,该方法包括将(S)-3-((3,5-二甲氧基苯基)乙炔基)-1-(吡咯烷-3-基)-1H-吡唑并[3,4-D]嘧啶-4-胺或其盐与化学式(I-1-A)表示的化合物反应.化学式(I-1-A)和化学式(A-1)如说明书中所述.
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2901292000-乙炔
2902300000-甲苯 - 💡 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-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.
专利号:WO-2025137620-A1
优先权日:2023-12-21
标题:Methods for high quality and high accuracy methylation sequencing
发明人：KENNEDY ANDREW
权利人:GUARDANT HEALTH INC
摘要:Provided herein are methods and compositions for calibrating one or more base calling metrics in a sequencing by synthesis reaction, and for calling at least a portion of nucleobases in a converted region of a DNA molecule using the one or more calibrated base calling metrics. Provided herein are also methods for determining the likelihood that a subject has a disease or condition, such as cancer.
专利号:CN-115785103-A
优先权日:2022-12-28
标题 :A kind of synthesis method of Fabatinib for treating cholangiocarcinoma
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: Matranga G, Carollo A, Alaimo M, Cutaia S, Rizzo S, Provenzani A. Safety profiles of the new target therapies-pemigatinib, futibatinib, and ivosidenib- for the treatment of cholangiocarcinoma: a systematic review. Ther Adv Drug Saf. 2025 Aug 19;16:20420986251347376. doi: 10.1177/20420986251347376.
2: Pirozzi A, Hoyek C, Okano N, Abidoye O, Rimassa L, Sonbol MB, Uson Junior PLS, Bekaii-Saab T, Borad MJ. Pharmacologic features, clinical applications, and drug safety evaluation of futibatinib in the treatment of biliary tract cancer (BTC). Expert Opin Drug Saf. 2025 Dec;24(12):1383-1390. doi: 10.1080/14740338.2025.2495178. Epub 2025 May 1. 2024 Sep 11. 19(3):473-480. doi: 10.1007/s11523-024-01059-8. Epub 2024 May 9. 28(11):928-943. doi: 10.1093/oncolo/oyad149.
6: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Futibatinib. 2023 May 15. 2012–. Futibatinib. 2022 Nov 30. 82(18):1737-1743. doi: 10.1007/s40265-022-01806-z. 30(4):317-324. doi: 10.1080/13543784.2021.1837774. Epub 2020 Oct 25.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).
参考文献:10.1007/s12029-021-00637-7
摘要:Huang P, Zhou Y, Chen Y. Significant Response to Camrelizumab Plus Targeted Drugs in Recurrent Intrahepatic Cholangiocarcinoma: a Case Report and Literature Review. Journal of Gastrointestinal Cancer. 2021 Jul 26;53(3):817–24. doi: 10.1007/s12029-021-00637-7.
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