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溶解性：不确定。",{"pictogram":242,"signal":243,"hazards":244},"Irritant","Warning",[245,246,247,248],"H302 — Harmful if swallowed \u002F 吞咽有害","H315 — Causes skin irritation \u002F 造成皮肤刺激","H319 — Causes serious eye irritation \u002F 造成严重眼刺激","H335 — May cause respiratory irritation \u002F 可能造成呼吸道刺激",[],[251,254,257,260,263,266,269,272],{"key":252,"value":253},"描述","Gefitinib 是一种有效的表皮生长因子受体 (EGFR) 抑制剂,在 NR6wtEGFR 细胞中 IC50 值为 2-37 nM。",{"key":255,"value":256},"相关类别","信号通路\n>>\n自噬\n>>\n自噬\n信号通路\n>>\nJAK\u002FSTAT信号通路\n>>\nEGFR\n信号通路\n>>\n蛋白酪氨酸激酶\n>>\nEGFR\n研究领域\n>>\n癌症",{"key":258,"value":259},"靶点","EGFR",{"key":261,"value":262},"体外研究","吉非替尼(0.01-0.1mM)导致受体的磷酸酪氨酸负荷增加,ERK信号传导增加和刺激增殖和锚定非依赖性生长,可能是通过在EGFRvIII表达细胞的长期暴露中诱导EGFRvIII二聚化。另一方面,吉非替尼(1-2 mM)显着降低EGFRvIII磷酸酪氨酸负荷,EGFRvIII介导的增殖和不依赖贴壁的生长[1]。吉非替尼(ZD1839)抑制这些EGF驱动的未转化细胞的单层生长,IC50为20 nM [2]。吉非替尼可抑制CALU-3和GLC82细胞增殖,IC50为2μM[3]。",{"key":264,"value":265},"体内研究","与二甲双胍混合的吉非替尼(150mg\u002Fkg,口服)诱导携带H1299或CALU-3 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Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.\n[2].\nMoasser MM, et al. The tyrosine kinase inhibitor ZD1839 (\"Iressa\") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8.\n[3].\nMorgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19.\n[4].\nMiyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85.\n[5].\nNoh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS\u002FMS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27.\n[6].\nDhar D, et al. 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General tariff:20.0%",[340,343,345,348,351,354,357,360,363,366,369],{"key":341,"value":342},"符号","GHS07",{"key":344,"value":243},"信号词",{"key":346,"value":347},"危害声明","H302-H315-H319-H335",{"key":349,"value":350},"警示性声明","P301 + P312 + P330-P305 + P351 + P338",{"key":352,"value":353},"危害码 (欧洲)","Xi",{"key":355,"value":356},"风险声明 (欧洲)","R36\u002F37\u002F38:Irritating to eyes, respiratory system and skin .",{"key":358,"value":359},"安全声明 (欧洲)","S24\u002F25",{"key":361,"value":362},"危险品运输编码","NONH for all modes of transport",{"key":364,"value":365},"WGK德国","3",{"key":367,"value":368},"RTECS号","HP1149700",{"key":328,"value":370},"29143900","\u003Cp>1. 4-(3'-氯-4'-氟苯氨基)-6-羟基-7-甲氧基喹唑啉、3-吗啉基丙基氯、碳酸钾溶于二甲基甲酰胺中，搅拌反应。再加入3-吗啉基丙基氯，搅拌、过滤，滤液浓缩，得到的物质经柱层析，用4∶1的乙酸乙醇甲醇洗脱，得到的固体再用甲苯重结晶，得格非替尼。\u003Cbr \u002F>2. 6,7-二甲氧基-3H-喹唑啉-4-酮的制备\u003C\u002Fp>\u003Cp>在单口圆底反应瓶中加入2-氨基-4,5-二甲氧基苯甲酸30g(0.15mol)、盐酸甲脒48g(0.60mol)(经粉碎至40目),充分混合均匀,室温下于旋转蒸发器缓缓抽至真空后将抽气口夹死,50r\u002Fmin的速度下油浴加热至210ºC,反应混合物完全熔融后,将转速提至150r\u002Fmin,反应45min.冷却至80ºC,加0.33mol\u002FLNaOH溶液15ml,冷至室温,抽滤,滤饼用水洗,70ºC真空干燥,得6,7-二甲氧基-3H-喹唑啉-4-酮28g,为烟灰色固体,收率89.5%,mp>250ºC(文献[3]报道mp295~298ºC,收率79%).\u003C\u002Fp>\u003Cp>3. 6-羟基-7-甲氧基-3H-喹唑啉-4-酮的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入经无水MgSO4干燥24h的无水甲磺酸80ml(266.6g,2.77mol)和L-蛋氨酸40g(0.268mol),于40ºC搅拌下分批加入6,7-二甲氧基-3H-喹唑啉-4-酮26.5g(≈0.128mol).加毕,同温度下搅拌反应8h.冷至室温,搅拌下缓缓倾入750ml水中,抽滤,滤饼水洗至中性,得灰白色固体.加水300ml,加热至回流,趁热过滤,抽干,干燥,得6-羟基-7-甲氧基-3H-喹唑啉-4-酮9g,收率36.4%,mp200ºC(文献[3]报道收率36.6%)\u003C\u002Fp>\u003Cp>4. 6-乙酰氧基-7-甲氧基-3H-喹唑啉-4-酮的制备\u003Cbr \u002F>在反应瓶中加入6-羟基-7-甲氧基-3H-喹唑啉-4-酮14g(0.073mmol)、乙酸酐110ml(118.8g,1.164mol)和三氟化硼乙醚络合物3ml(3.38g,0.024mol),于40ºC搅拌反应4h.将反应液倾入200ml冰水中,抽滤,滤饼用水洗净,干燥,得白色粉末状物6-乙酰氧基-7-甲氧基-3H-喹唑啉-4-酮16.5g,收率95.6%,mp>200ºC.\u003C\u002Fp>\u003Cp>5. 6-乙酰氧基-4-氯-7-甲氧基喹唑啉盐酸盐的制备\u003Cbr \u002F>在反应瓶中加入6-乙酰氧基-7-甲氧基-3H-喹唑啉-4-酮15g(0.064mol)和DMF100ml,搅拌,加二氯亚砜10ml(0.14mol),搅拌升温至70ºC,搅拌反应6h.减压浓缩得到黏稠浆状物,室温搅拌下向其中缓缓加入冰水50ml,抽滤,得疏松颗粒状淡咖啡色固体.将固体于60ºC真空干燥后粉碎,加甲苯200ml,回流1h.冷却,过滤,干燥得土黄色固体6-乙酰氧基-4-氯-7-甲氧基喹唑啉盐酸盐16g,收率88%,mp>200ºC.\u003C\u002Fp>\u003Cp>6. 6-乙酰氧基-4-(3-氯-4-氟苯)氨基-7-甲氧基喹唑啉盐酸盐的制备\u003Cbr \u002F>在反应瓶中加入6-乙酰氧基-4-氯-7-甲氧基喹唑啉盐酸盐18.5g(0.064mol)、3-氯-4-氟苯胺9.5g(0.065mol)和异丙醇420mol,于90ºC回流搅拌反应5~6h.搅拌自然冷却至室温,抽滤,滤饼依次用异丙醇、甲醇洗涤,60ºC真空干燥,得淡米黄色粉末状固体6-乙酰氧基-4-(3-氯-4-氟苯)氨基-7-甲氧基喹唑啉盐酸盐14.5g,收率52.1%,mp>200ºC,(文献[3]报道收率56%)\u003C\u002Fp>\u003Cp>7. 4-(3-氯-4-氟苯)氨基-6-羟基-7-甲氧基喹唑啉的制备\u003Cbr \u002F>在反应瓶中加入6-乙酰氧基-4-(3-氯-4-氟苯)氨基-7-甲氧基喹唑啉盐酸盐10g(0.23mol)、5mol\u002FLNaOH水溶液20ml和甲醇200ml,于40ºC,搅拌反应6h.冷至室温,用0.1mpl\u002FL盐酸调pH5~6,抽滤,滤饼用甲醇洗,抽干,干燥,得白色鳞片状固体4-(3-氯-4-氟苯)氨基-6-羟基-7-甲氧基喹唑啉7g,收率95.2%.\u003C\u002Fp>\u003Cp>8.1-(3-氯丙基)吗啉的制备\u003Cbr \u002F>在反应瓶中加入吗啉72g(0.46mol)、1-氯-3-溴丙烷60g(0.69mol)、苯400ml和无水K2CO3 70g(0.51mol),室温搅拌1h.缓慢升温至沸(微沸),在该温度搅拌反应1.5h.继续升至回流,回流反应3h.冷却,抽滤,滤饼用无水乙醚洗涤.合并滤液和洗液(黄色),用3mol\u002FL盐酸(150ml×3)提取,弃去有机相,水相用10mol\u002FLNaOH溶液调至pH10.分出黄色油层,层用乙醚提取3次,合并提取液,无水K2CO3干燥,过滤,滤液减压除去溶剂,得黄色粗品油状物50.0g,减压蒸馏,收集57~60ºC\u002F400Pa馏分,得无色液体42.9g,收率57.3%.\u003C\u002Fp>\u003Cp>9. N-(3-氯-4-氟苯基)-7-甲氧基-6-[3-(4-吗啉基)-丙氧基]-4-喹唑啉基胺(吉非替尼)的合成\u003C\u002Fp>\u003Cp>在反应瓶中加入1-(3-氯丙基)吗啉10g(31.3mmol)和DMF适量,搅拌溶解,于<5ºC加入等物质的量的NaOH,搅拌反应0.5h.得到稀粥状液体.向其中滴加5.2g(31.3mmol)1-(3-氯丙基)吗啉溶于300ml氯仿的溶液,约4h滴完.室温下搅拌反应4h.减压蒸除溶剂.剩余物用300ml热的甲苯溶解,活性炭脱色,热过滤,缓慢冷却滤液,析晶,过滤,得浅黄绿色固体7.5g(再次脱色重结晶可得浅黄色固体),收率58.1%,mp117~119ºC.,(文献[3]报道mp119~120ºC,收率50%)\u003C\u002Fp>","2026-08-21T07:51:12.859463Z",false,[375,380,386,392,398,404],{"slug":376,"cid":377,"name":378,"nameZh":378,"cas":379},"785947418393841664","J-1874835-6","((Perfluorohexyl)ethyl)-2-chloropropenoate","96383-55-0",{"slug":381,"cid":382,"name":383,"nameZh":384,"cas":385},"785891221192052736","J-1095551-6","Sudan Black B","苏丹黑B","4197-25-5",{"slug":387,"cid":388,"name":389,"nameZh":390,"cas":391},"785876430910132224","J-1352432-0","Carbasalate calcium","卡巴匹林钙","93803-83-9",{"slug":393,"cid":394,"name":395,"nameZh":396,"cas":397},"785891455125164032","J-29802-1","Pigment Red 48:2","颜料红48:2","7023-61-2",{"slug":399,"cid":400,"name":401,"nameZh":402,"cas":403},"785895952778006528","J-1512648-7","Pigment Red 52:1","颜料红52:1","17852-99-2",{"slug":405,"cid":406,"name":407,"nameZh":408,"cas":409},"785875705589141504","J-10742-4","Neocuproine hemihydrate","新亚铜试剂半水合物","34302-69-7",1792622396185,"zh-CN",[]]