CAS: 849217-64-7; N-(3-Fluoro-4-((6-Methoxy-7-(3-Morpholinopropoxy)Quinolin-4-yl)Oxy)Phenyl)-N-(4-Fluorophenyl)Cyclopropane-1,1-Dicarboxamide
该化合物是一种小分子抑制剂,主要针对受体强力强力性血管,特别是MET和VEGFR2,它们涉及扩散,生存和血管产生等各种细胞过程,被归类为实验性抗癌剂,并因其在治疗各种恶性肿瘤,包括肾细胞癌和其他固态肿瘤方面的潜力而受到调查.Foretinib 展示了一种独特的化学结构,允许它干扰与肿瘤生长和转移有关的信号路径.该化合物通常通过口述方式管理,并在临床试验中评估其功效和安全性能.其行动机制包括阻止特定抗生素残留物的磷化,从而抑制下游信号级,以促进癌症细胞生存和扩散.与许多有针对性的疗法一样,Foretinib的效力可能因肿瘤的遗传和分子特性而不同,突出个人化医学在肿瘤学中的重要性.
- 英文名称N-(3-Fluoro-4-((6-Methoxy-7-(3-Morpholinopropoxy)Quinolin-4-yl)Oxy)Phenyl)-N-(4-Fluorophenyl)Cyclopropane-1,1-Dicarboxamide
- 中文名称2-溴-1-(4-氟苯基)-1-丁酮
- IUPAC名称N-(3-fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
- 其它别名Foretinib; N-[3-Fluoro-4-[[6-(methyloxy)-7-[[3-(morpholin-4-yl)propyl]oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
- CAS编号849217-64-7
- MFCD编号:MFCD16038048
- EINECS号:629-893-0
- FDA UNII编号:81FH7VK1C4
- 分子式:C34H34F2N4O6
- 分子量:632.66
- 产品CID: 1840642
- 同类组份化合物CAS1226999-07-0 (phosphate)849217-64-7 (free base)
- 产品分类生物化工 → 抑制剂 → 蛋白酪氨酸激酶
物理性质
- 熔点>98°C (分解)
- 沸点828.5±65.0 °C at 760 mmHg
- 闪点454.8±34.3 °C
- 密度1.4±0.1 g/cm3
- pKa:13.14±0.70(预测)
- PSA:116.45
- LogP:5.12
- 折射率1.649
- 蒸汽压0.0±3.0 mmHg at 25°C
- 溶解性DMSO (Slightly), Ethanol (Slightly)
- 外观形态淡黄色至黄色黄色粉末
- 储存条件密封干燥,冷冻保存, 低于 -20°C
- 产品应用该化合物是HGFR(MET)和VEGFER(VEGBFR)的ATP竞争抑制剂,主要针对MET和KDR, 其IC50值分别为0.4纳米M和0.9纳米M;它处于治疗癌症的第二阶段临床调查之下;它通过阻塞与肿瘤血管血管扩张有关的超常HGGF/MET信号和多重受体强体强血酶酶,包括RON,FLT-1/3/4,KIT,PDGFFRA/Β和TIE-2. FRETEINIB在各种前临床模型中表现出强大的抗扰动活动,诱发肿瘤出出出血红肿,坏球,并全面回归人类基因移植.它抑制了癌症细胞系中的聚体形成(例如B16F10,A549,HT29)和气态癌症模型中不同抑制细胞生长(MKN-45和KATTO-III),它显著降低了MIN V.
MSDS等安全信息
欧盟法规
ECHA物质C&L通报上下游产品
CAS号849217-48-7 1-(4-氟苯基氨基甲酰基)环丙烷羧酸 | CAS号849217-50-1 N1'-[3-fluoro-4... | CAS号57616-74-7 4-(3-氯丙基)吗啉盐酸盐 | CAS号849217-58-9 N-(3-fluoro-4-h...合成工艺路线路线简述
- 849217-48-7 + 479690-10-3 = 849217-64-7
反应条件:1.1 Reagents: Diisopropylethylamine,O-(7-Azabenzotriazol-1-Yl)-N,N,N′,N′-Tetramethyluronium Hexafluorophosphate Solvents: Dimethylformamide; 18 H,Rt
标题:Synthesis Of A Small Molecular Inhibitor Of C-Met,Xl880
作者:Yan,Jiaju; Liu,Jing; Wang,Lin; Zhang,Shouguo; Yan,Haiyan; Et Al
参考文献:Zhongguo Xinyao Zazhi 日期:2012 卷标:21(9) 页码:1042-1045
7-苄氧基-4-羟基-6-甲氧基喹啉置于palladium 10% On Activated Carbon 2,6-二甲基吡啶,4-二甲氨基吡啶,1,4-环己二烯,Potassium Carbonate体系中,用 乙醇,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 17.75H,反应生成 N-[3-氟-4-[[6-甲氧基-7-[[3-(吗啉-4-基)丙基]氧]喹啉-4-基]氧]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺
参考文献: C-Met Modulators And Methods Of Use[fr] Modulateurs De C-Met Et Procede D'Utilisation
标题: C-Met Modulators And Methods Of Use[fr] Modulateurs De C-Met Et Procede D'Utilisation
海关参考信息
- 2905121000-正丙醇
2907210001-间苯二酚
2909110000-乙醚
2912110000-甲醛 - 💡 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.
专利号:US-2024400576-A1
优先权日:2021-09-03
标 题:Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof
发明人：RODRIGUEZ RAPHAËL; CZERWONKA DOMINIKA; ANTOSZCZAK MICHAL; HUCZYNSKI ADAM
权利人:CENTRE NAT RECH SCIENT; INST CURIE; INST NAT SANTE RECH MED; ADAM MICKIEWICZ UNIV
摘要:The present invention relates to nitrogen-containing derivatives of salinomycin having the formula (I), as well as pharmaceutically acceptable salt thereof, and synthesis and uses thereof, in particular for the treatment and/or prevention of cancer including for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.
专利号:US-2025250280-A1
优先权日:2021-09-03
标 题 :Nitrogen-containing derivatives of narasin, synthesis and uses thereof
发明人：RODRIGUEZ RAPHAËL; CAÑEQUE TATIANA; MÃœLLER SEBASTIAN; ANTOSZCZAK MICHAL
权利人:CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; INST CURIE
摘要:The present invention relates to nitrogen-containing derivatives of narasin having the formula (I), as well as synthesis and uses thereof, in particular for the treatment and/or prevention of cancer. Also disclosed are medicaments including the nitrogen-containing derivatives of narasin, which include medicaments for preventing cancer metastasis and/or for preventing cancer recurrence and/or for decreasing resistance to a chemotherapy in a subject.
专利号:WO-2023031399-A1
优先权日:2021-09-03
标题 :Iron-activable nitrogen-containing derivatives of salinomycin and narasin, synthesis and use for the treatment of cancers
专利号:WO-2023031402-A1
优先权日:2021-09-03
标 题 :Nitrogen-containing derivatives of salinomycin, synthesis and uses thereof
专利号:WO-2023031362-A1
优先权日:2021-09-03
标题:Nitrogen-containing derivatives of narasin, synthesis and uses thereof
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主要参考文献
1: Daeschler SC, Zhang J, Gordon T, Borschel GH, Feinberg K. Foretinib mitigates cutaneous nerve fiber loss in experimental diabetic neuropathy. Sci Rep. 2022 May 19;12(1):8444. doi: 10.1038/s41598-022-12455-3.
2: Fujino T, Suda K, Koga T, Hamada A, Ohara S, Chiba M, Shimoji M, Takemoto T, Soh J, Mitsudomi T. Foretinib can overcome common on-target resistance mutations after capmatinib/tepotinib treatment in NSCLCs with MET exon 14 skipping mutation. J Hematol Oncol. 2022 Jun 11;15(1):79. doi: 10.1186/s13045-022-01299-z.
3: Gortany NK, Panahi G, Ghafari H, Shekari M, Ghazi-Khansari M. Foretinib induces G2/M cell cycle arrest, apoptosis, and invasion in human glioblastoma cells through c-MET inhibition. Cancer Chemother Pharmacol. 2021 Jun;87(6):827-842. doi: 10.1007/s00280-021-04242-0. Epub 2021 Mar 10. 9(32):22769-22784. doi: 10.18632/oncotarget.25232.
合成参考文献
参考文献:10.1158/0008-5472.can-10-2527
摘要:You WK, Sennino B, Williamson CW, Falcón B, Hashizume H, Yao LC, Aftab DT, McDonald DM. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res. 2011 Jul 15;71(14):4758–68.
参考文献:10.1016/j.bmc.2014.05.013
摘要:Liu Z, Wang R, Guo R, Hu J, Li R, Zhao Y, Gong P. Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors. Bioorg Med Chem. 2014 Jul 15;22(14):3642–53. doi: 10.1016/j.bmc.2014.05.013.
参考文献:10.1186/s12885-015-1737-4
摘要:Lee KH, Lee KB, Kim TY, Han SW, Oh DY, Im SA, Kim TY, Yi NJ, Lee KW, Suh KS, Jang JJ, Bang YJ. Clinical and pathological significance of ROS1 expression in intrahepatic cholangiocarcinoma. BMC Cancer. 2015 Oct 16;15():721.
参考文献:10.1007/s10565-019-09483-7
摘要:Lee CH, Decker AM, Cackowski FC, Taichman RS. Bone microenvironment signaling of cancer stem cells as a therapeutic target in metastatic prostate cancer. Cell Biology and Toxicology. 2019 Jun 27;36(2):115–30. doi: 10.1007/s10565-019-09483-7.
参考文献:10.1007/s00280-019-03902-6
摘要:Roys A, Chang X, Liu Y, Xu X, Wu Y, Zuo D. Resistance mechanisms and potent-targeted therapies of ROS1-positive lung cancer. Cancer Chemother Pharmacol. 2019 Oct;84(4):679–88. doi: 10.1007/s00280-019-03902-6.
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