CAS: 1393466-87-9; (R)-N-(3-(5-(2-Cyclopropylpyrimidin-5-yl)-1H-Pyrrolo[2,3-B]Pyridine-3-Carbonyl)-2,4-Difluorophenyl)-3-Fluoropyrrolidine-1-Sulfonamide
- 英文名称(R)-N-(3-(5-(2-Cyclopropylpyrimidin-5-yl)-1H-Pyrrolo[2,3-B]Pyridine-3-Carbonyl)-2,4-Difluorophenyl)-3-Fluoropyrrolidine-1-Sulfonamide
- 中文名称化合物PLX8394
- IUPAC名称(R)-N-(3-(5-(2-cyclopropylpyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)-3-fluoropyrrolidine-1-sulfonamide
- 其它别名Plixorafenib; (R)-N-(3-(5-(2-Cyclopropylpyrimidin-5-yl)-1H-Pyrrolo[2,3-B]Pyridine-3-Carbonyl)-2,4-Difluorophenyl)-3-Fluoropyrrolidine-1-Sulfonamide; (3R)-N-[3-[5-(2-Cyclopropylpyrimidin-5-
- CAS编号1393466-87-9
- MFCD编号:MFCD29472263
- FDA UNII编号:J2L7Z273SG
- 分子式:C25H21F3N6O3S分子量:542.54
- 产品CID: 609328
- 同类组份化合物CAS1393466-87-9
- 产品分类生物化工 → 生化试剂 → 激动剂抑制剂
物理性质
- 沸点786.8±70.0°C at 760 mmHg
- 密度1.60±0.1 g/cm3(预测)
- LogP:2.8
- 溶解性DMSO:≥ 39 mg/mL (71.89 mM);水:< 0.1 mg/mL(不溶)
- 外观形态白色 至类白色 固体-粉末
- 储存条件Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
- 产品应用该化合物是一种口服活性小型分子BRAF抑制剂,具有潜在的抗振活动;它以IC50值分别为3.8纳米,14纳米和23纳米,抑制BRAW(V600E),野型BRAFF和CRAF;它不会引起RAF/MEK/ERK路径和BRAV单质块的自相矛盾的激活.
上下游产品
(3-氨基-2,6-二氟苯基)(5-溴-1H-吡咯并[2,3-B]吡啶-3-基)甲酮 (3-Amino-2,6-Difluorophenyl)(5-Bromo-1H-Pyrrolo[2,3-B]Pyridin-3-yl)Methanone 1312941-98-2(3-Amino-2,6-Difluorophenyl)-[5-Bromo-1-(2,6-Dichlorobenzoyl)Pyrrolo[2,3-B]Pyridin-3-Yl]Methanone
合成工艺路线路线简述
📜5-溴-7-氮杂吲哚置于吡啶,甲醇,4-二甲氨基吡啶,Aluminum (III) Chloride,Bis-Triphenylphosphine-Palladium(II) Chloride,氨,碳酸氢钠,三乙胺,Tin(Ll) Chloride体系中,用 四氢呋喃,2-甲基四氢呋喃,二氯甲烷 用作溶剂,化学反应生成化合物plx8394
参考文献:Solid Forms Of A Compound For Modulating Kinases
标题:Solid Forms Of A Compound For Modulating Kinases
摘要:化合物i的固体形式(及其s-对映体,化合物ii),对蛋白激酶具有活性,已经制备并表征: 还提供了使用这些固体形式的方法.
海关参考信息
- 2912110000-甲醛
2912210000-苯甲醛
2933310010-吡啶
2914190090-其他无环酮 - 💡 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-9994567-B2
优先权日:2015-05-22
标 题:Synthesis of heterocyclic compounds
发明人：IBRAHIM PRABHA N; LIN JACK; SPEVAK WAYNE; ZHANG JIAZHONG
权利人:PLEXXIKON INC
摘要:Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): n nor a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P 1 and P 2 are as defined in this disclosure.
专利号:US-2018002332-A1
优先权日:2015-05-22
标题 :Synthesis of heterocyclic compounds
专利号:EP-3298012-B1
优先权日:2015-05-22
标题:Synthesis of heterocyclic compounds
专利号:TW-I658042-B
优先权日:2015-05-22
标 题:Synthesis of heterocyclic compounds
专利号:US-2016340358-A1
优先权日:2015-05-22
标题 :Synthesis of heterocyclic compounds
专利号:JP-6722200-B2
优先权日:2015-05-22
标题 :Synthesis of heterocyclic compounds
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: Geisen ME, Tessmann JW, Kelson CO, He D, Wang C, Faisal ASM, Beswick EJ, Baca Y, Rock S, Kolesar JM, Zaytseva YY. Inhibition of fatty acid synthase enhances therapeutic efficacy and delays acquired resistance to BRAF-targeted therapy in colorectal cancer. Neoplasia. 2026 Mar;73:101283. doi: 10.1016/j.neo.2026.101283. Epub 2026 Feb 5.
2: Yi JS, McCarthy KS, Mazur K, Kudlaty R, Armstrong T, Desai N, Shepherd SP, Zinn D, Velazquez J, Scull B, Allen C, McClain K. Sustained Response to Pan-BRAF Inhibitor Plixorafenib (FORE8394, PLX8394) in a Young Adult With Neurodegenerative Langerhans Cell Histiocytosis. JCO Precis Oncol. 2025 Oct;9:e2500225. doi: 10.1200/PO-25-00225. Epub 2025 Oct 9.
3: Lavoie H, Jin T, Lajoie D, Decossas M, Gendron P, Wang B, Filandr F, Sahmi M, Hwa Jo C, Weber S, Arseneault G, Tripathy S, Beaulieu P, Schuetz DA, Schriemer DC, Marinier A, Rice WJ, Maisonneuve P, Therrien M. BRAF oncogenic mutants evade autoinhibition through a common mechanism. Science. 2025 May 29;388(6750):eadp2742. doi: 10.1126/science.adp2742. Epub 2025 May 29. 15(5):2035-2051. doi: 10.7150/thno.103958.
合成参考文献
参考文献:10.1038/nature14982
摘要:Zhang C, Spevak W, Zhang Y, Burton EA, Ma Y, Habets G, Zhang J, Lin J, Ewing T, Matusow B, Tsang G, Marimuthu A, Cho H, Wu G, Wang W, Fong D, Nguyen H, Shi S, Womack P, Nespi M, Shellooe R, Carias H, Powell B, Light E, Sanftner L, Walters J, Tsai J, West BL, Visor G, Rezaei H, Lin PS, Nolop K, Ibrahim PN, Hirth P, Bollag G. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015 Oct 22;526(7574):583–6. doi: 10.1038/nature14982.
📝 需求与反馈
尽可能描述清楚需求与问题信息
