[{"data":1,"prerenderedAt":-1},["ShallowReactive",2],{"currency-rates":3,"$fyk2oeqxpb7bd":8,"compound-J-1961711-9":169,"verified-suppliers-J-1961711-9":392},{"rates":4,"source":7},{"USD":5,"CNY":6},1,6.679814,"live",{"rows":9,"total":167,"current":5,"size":168},[10,33,45,60,73,84,96,111,121,133,145,156],{"slug":11,"cid":12,"imgSvg":13,"name":14,"nameZh":15,"cas":16,"formula":17,"iupac":14,"category":18,"categoryName":19,"categoryEnName":20,"industry":21,"tags":22,"offersCount":24,"supplierCount":25,"bestOffer":26},"843627791009189888","J-1971488-6","\u002Fimages\u002Fchem_structures_svg\u002F399\u002F65845-61-6.svg","N-Methylcyclohexanamine hydrochloride","N-甲基环己胺盐酸盐","65845-61-6","C7H16ClN","acids","有机酸","Organic Acids","",[23],"In Stock",4,2,{"unitPrice":27,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},2.64,"500g","CNY","China","CN","in-stock",{"slug":34,"cid":35,"imgSvg":36,"name":37,"nameZh":38,"cas":39,"formula":40,"iupac":37,"category":18,"categoryName":19,"categoryEnName":20,"industry":21,"tags":41,"offersCount":24,"supplierCount":5,"bestOffer":42},"785882541994283008","J-1323843-2","\u002Fimages\u002Fchem_structures_svg\u002F104\u002F67627-18-3.svg","Potassium indigotrisulfonate","靛蓝三磺酸钾","67627-18-3","C16H7K3N2O11S3",[23],{"unitPrice":43,"pack":44,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},180,"5g",{"slug":46,"cid":47,"imgSvg":48,"name":49,"nameZh":50,"cas":51,"formula":52,"iupac":49,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":56,"offersCount":57,"supplierCount":25,"bestOffer":58},"785889752443260928","J-28559-6","\u002Fimages\u002Fchem_structures_svg\u002F292\u002F15060-55-6.svg","Ammonium tetrathiomolybdate","四硫钼酸铵","15060-55-6","H8MoN2S4","inorganic","无机化合物","Inorganic Chemicals",[23],10,{"unitPrice":59,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},24,{"slug":61,"cid":62,"imgSvg":63,"name":64,"nameZh":65,"cas":66,"formula":67,"iupac":64,"category":18,"categoryName":19,"categoryEnName":20,"industry":21,"tags":68,"offersCount":69,"supplierCount":25,"bestOffer":70},"855452191530422272","J-1994428-6","\u002Fimages\u002Fchem_structures_svg\u002F500\u002F16350-96-2.svg","N-benzylcyclohexanamine.hydrochloride","N-苄基环己胺盐酸盐","16350-96-2","C13H20ClN",[23],5,{"unitPrice":71,"pack":28,"currency":29,"origin":72,"originFlag":31,"moq":21,"stock":32},6,"中国",{"slug":74,"cid":75,"imgSvg":76,"name":77,"nameZh":78,"cas":79,"formula":80,"iupac":77,"category":18,"categoryName":19,"categoryEnName":20,"industry":21,"tags":81,"offersCount":25,"supplierCount":25,"bestOffer":82},"785871840001134592","J-982001-3","\u002Fimages\u002Fchem_structures_svg\u002F001\u002F10517-44-9.svg","1,3-Diaminopropane dihydrochloride","1,3-二氨基丙烷二盐酸盐","10517-44-9","C3H12Cl2N2",[23],{"unitPrice":83,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},3.78,{"slug":85,"cid":86,"imgSvg":87,"name":88,"nameZh":89,"cas":90,"formula":91,"iupac":88,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":92,"offersCount":93,"supplierCount":94,"bestOffer":95},"785880365658017792","J-14975-7","\u002Fimages\u002Fchem_structures_svg\u002F262\u002F12003-67-7.svg","Lithium aluminate","氧化铝锂","12003-67-7","AlLiO2",[23],7,3,{"unitPrice":94,"pack":28,"currency":29,"origin":72,"originFlag":31,"moq":21,"stock":32},{"slug":97,"cid":98,"imgSvg":99,"name":100,"nameZh":101,"cas":102,"formula":103,"iupac":100,"category":104,"categoryName":105,"categoryEnName":106,"industry":21,"tags":107,"offersCount":94,"supplierCount":5,"bestOffer":109},"785871830249377792","J-6931-8","\u002Fimages\u002Fchem_structures_svg\u002F456\u002F58068-80-7.svg","1-Octanoylbenzotriazole","N-辛酰苯并三唑","58068-80-7","C14H19N3O","aromatics","芳香烃","Aromatic Hydrocarbons",[108],"Made to Order",{"unitPrice":110,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},0.56,{"slug":112,"cid":113,"imgSvg":114,"name":115,"nameZh":116,"cas":117,"formula":118,"iupac":115,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":119,"offersCount":69,"supplierCount":25,"bestOffer":120},"785871842446413824","J-1960944-0","\u002Fimages\u002Fchem_structures_svg\u002F495\u002F10534-86-8.svg","Hexaamminecobalt(III) nitrate","六氨合钴(III)硝酸盐","10534-86-8","CoH18N9O9",[23],{"unitPrice":71,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},{"slug":122,"cid":123,"imgSvg":124,"name":125,"nameZh":126,"cas":127,"formula":128,"iupac":125,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":129,"offersCount":24,"supplierCount":25,"bestOffer":130},"785871842576437248","J-814544-6","\u002Fimages\u002Fchem_structures_svg\u002F221\u002F12037-42-2.svg","vanadium oxide","氧化钒","12037-42-2","O13V6",[23],{"unitPrice":131,"pack":132,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},112.8,"100g",{"slug":134,"cid":135,"imgSvg":136,"name":137,"nameZh":138,"cas":139,"formula":140,"iupac":137,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":141,"offersCount":142,"supplierCount":5,"bestOffer":143},"785871842647740416","J-1333345-4","\u002Fimages\u002Fchem_structures_svg\u002F479\u002F26490-63-1.svg","COBALT TETRAFLUOROBORATE HEXAHYDRATE","四氟化硼钴水合物","26490-63-1","B2CoF8H12O6",[23],8,{"unitPrice":144,"pack":132,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},11,{"slug":146,"cid":147,"imgSvg":148,"name":149,"nameZh":150,"cas":151,"formula":152,"iupac":149,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":153,"offersCount":57,"supplierCount":94,"bestOffer":154},"785871842698072064","J-814953-9","\u002Fimages\u002Fchem_structures_svg\u002F432\u002F72259-10-0.svg","Copper(II) tetrafluoroborate hexahydrate","六水合四氟硼酸铜(II)","72259-10-0","B2CuF8H12O6",[23],{"unitPrice":155,"pack":28,"currency":29,"origin":21,"originFlag":21,"moq":21,"stock":32},2.6,{"slug":157,"cid":158,"imgSvg":159,"name":160,"nameZh":161,"cas":162,"formula":163,"iupac":160,"category":53,"categoryName":54,"categoryEnName":55,"industry":21,"tags":164,"offersCount":94,"supplierCount":5,"bestOffer":165},"785871863254355968","J-1990080-2","\u002Fimages\u002Fchem_structures_svg\u002F149\u002F123333-60-8.svg","Cerium(IV) sulfate hydrate","铈(IV)硫酸盐水合物","123333-60-8","CeH2O9S2",[108],{"unitPrice":166,"pack":28,"currency":29,"origin":30,"originFlag":31,"moq":21,"stock":32},5.6,3204,12,{"slug":170,"cid":171,"imgSvg":172,"name":173,"nameZh":174,"cas":175,"formula":176,"iupac":173,"mdl":21,"mw":177,"category":178,"categoryName":179,"categoryEnName":180,"industry":21,"tags":181,"synonyms":182,"properties":186,"ghs":233,"offers":234,"activity":235,"upstream":263,"downstream":306,"customs":307,"safetyRows":308,"updatedAt":315,"isProhibited":316,"related":317,"__ts":390,"__lang":391,"__slug":171},"785892735537123328","J-1961711-9","\u002Fimages\u002Fchem_structures_svg\u002F302\u002F698387-09-6.svg","Neratinib","来那替尼","698387-09-6","C30H29ClN6O3","557.043","organic","有机化合物","Organic Compounds",[],[183,184,185],"诺拉替尼","HKI-272","(2E)-N-[4-[[3-氯-4-[(吡啶-2-基)甲氧基]苯基]氨基]-3-氰基-7-乙氧基喹啉-6-基]-4-(二甲基氨基)丁-2-烯酰胺",[187,192,197,202,207,211,214,217,221,225,229],{"label":188,"labelZh":189,"value":190,"prop":191},"Melting Point","熔点","184 °C","meltingPoint",{"label":193,"labelZh":194,"value":195,"prop":196},"Boiling Point","沸点","757.0±60.0 °C at 760 mmHg","boilingPoint",{"label":198,"labelZh":199,"value":200,"prop":201},"Density","密度","1.3±0.1 g\u002Fcm3","density",{"label":203,"labelZh":204,"value":205,"prop":206},"Flash Point","闪点","411.6±32.9 °C","flashPoint",{"label":208,"labelZh":209,"value":210},"Exact Mass","精确质量","556.198975",{"label":212,"labelZh":212,"value":213},"PSA","112.40000",{"label":215,"labelZh":215,"value":216},"LogP","5.46",{"label":218,"labelZh":219,"value":220},"Appearance","外观性状","固体;White to Light yellow powder to crystal",{"label":222,"labelZh":223,"value":224},"Vapor Pressure","蒸汽压","0.0±2.5 mmHg at 25°C",{"label":226,"labelZh":227,"value":228},"Refractive Index","折射率","1.667",{"label":230,"labelZh":231,"value":232},"Storage Conditions","储存条件","\u003C0°C;避免加热",null,[],[236,239,242,245,248,251,254,257,260],{"key":237,"value":238},"描述","Neratinib 是一种可口服的,不可逆的 tyrosine kinase 抑制剂,能够抑制 HER2 和 EGFR 的活性,IC50 值分别为 59 nM 和 92 nM。",{"key":240,"value":241},"相关类别","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":243,"value":244},"靶点","EGFR:92 nM (IC50)\nHER2:59 nM (IC50)",{"key":246,"value":247},"体外研究","Neratinib对酪氨酸激酶KDR和Src具有抑制作用,IC50分别为0.8μM和1.4μM,与HER2相比,活性降低14倍和24倍。 Neratinib对其他丝氨酸-苏氨酸激酶没有活性,如Akt,细胞周期蛋白D1\u002Fcdk4,细胞周期蛋白E\u002Fcdk2,细胞周期蛋白B1\u002Fcdk1,IKK-2,MK-2,PDK1,c-Raf和Tpl-2,以及作为酪氨酸激酶c-Met。 Neratinib选择性抑制转染HER2(3T3\u002Fneu)的3T3细胞以及另外两种HER-2过表达SK-Br-3和BT474细胞的增殖,IC50值为2-3 nM,显示> 230倍与未转染的3T3细胞以及EGFR-和HER2-阴性的MDA-MB-435和SW620相比具有效力。 Neratinib还抑制EGFR依赖性A431细胞的增殖,IC50为81 nM。 Neratinib降低BT474细胞中HER2受体的自身磷酸化,IC50为5 nM,A431细胞中EGFR依赖于EGFR的磷酸化,IC50为3 nM。 Neratinib阻断HER-2导致下游MAPK和Akt通路的抑制,IC50为2 nM,比曲妥珠单抗更有效。 Neratinib抑制BT474细胞中细胞周期蛋白D1的表达和Rb易感基因的磷酸化,IC50为9 nM,导致G1-S停滞,最终导致细胞增殖减少[1]。",{"key":249,"value":250},"体内研究","口服治疗的neratinib显着抑制3T3\u002Fneu异种移植物的生长,分别在10,20,40和80mg\u002Fkg \u002F天的剂量下抑制34％,53％,98％和98％。与在40mg\u002Fkg \u002F天给药1小时内HER-2磷酸化抑制84％相一致,Neratinib在5,10的剂量下抑制BT-744异种移植物的生长70-82％,67％和93％ ,和40毫克\u002F千克\u002F天。 Neratinib对SK-OV-3异种移植物也有效,在5和60mg\u002Fkg \u002F天时分别抑制31％和85％。与HER-2依赖性肿瘤相比,Neratinib对EGFR依赖性A431异种移植物的效力较低,分别在5和20mg\u002Fkg \u002F天时具有32％和44％的抑制。 Neratinib对表达低水平HER-2和EGFR的MCF-7和MX-1异种移植物几乎没有活性,在80mg\u002Fkg \u002F天时仅有28％的抑制,表明Neratinib对表达HER-2或EGFR的细胞具有选择性活性。 [1]。",{"key":252,"value":253},"激酶实验","将Neratinib制备成DMSO中的10mg \u002F mL储液，并在25mM HEPES（pH7.5; 0.002ng \u002F mL-20μg\u002F mL）中稀释。将纯化的HER2重组COOH-末端片段（氨基酸676-1255）或表皮生长因子受体（EGFR）（氨基酸645-1186）[在100mM HEPES（pH7.5）和50％甘油中稀释]以增加的浓度温育Neratinib在4mM HEPES（pH7.5），0.4mMMnCl2,20μM钒酸钠和0.2mM DTT中在室温下在96孔ELISA板中15分钟。通过加入40μMATP和20mM MgCl 2引发激酶反应，并使其在室温下进行1小时。洗涤平板，并使用铕标记的抗磷酸酪氨酸抗体（15ng \u002F孔）检测磷酸化。在洗涤和增强步骤后，使用Victor2荧光读数器（激发波长340nm，发射波长615nm）检测信号。从抑制曲线计算抑制受体磷酸化50％的Neratinib浓度（IC 50）。",{"key":255,"value":256},"细胞实验","将细胞暴露于各种浓度的Neratinib 2或6天。使用磺酰罗丹明B（一种蛋白质结合染料）测定细胞增殖。简言之，将细胞用10％三氯乙酸固定并用水充分洗涤。然后将细胞用0.1％磺酰罗丹明B染色并在5％乙酸中洗涤。将蛋白质相关染料溶解于10mM Tris中，并在450nM下测量吸光度。从抑制曲线确定抑制细胞增殖50％的Neratinib浓度（IC 50）。",{"key":258,"value":259},"动物实验","将肿瘤细胞（维持在组织培养物中）或肿瘤片段皮下植入雌性无胸腺（裸）小鼠的侧腹。对于雌激素依赖性细胞系（BT474，MCF-7和SK-OV-3），在植入肿瘤前1周，给动物植入激素颗粒（0.72mg 17-β雌二醇，60天释放）。另外，将SK-OV-3细胞悬浮在Matrigel基底膜基质中用于植入。在将动物随机分配到不同治疗组（分期，第0天）后，在肿瘤达到90-200mg的大小后开始治疗。对于3T3 \u002F neu异种移植物，在肿瘤植入后第二天（第0天）开始治疗。 HKI-272在0.5％甲基纤维素-0.4％聚山梨醇酯-80（吐温80）中配制，并通过管饲法每日口服施用。每7天测定肿瘤质量[（长度×宽度2）\u002F 2]。除3T3 \u002F neu外，所有异种移植研究中的肿瘤生长表示为相对肿瘤生长：第0天平均肿瘤质量与平均肿瘤质量的比率。相对于载体处理的对照计算肿瘤生长的抑制。在数据的对数转换后使用单尾学生t检验（等方差）证明抑制的统计显着性。",{"key":261,"value":262},"参考文献","[1].\nRabindran SK, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res, 2004, 64(11), 3958-3965.\n[2].\nYoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176.",[264,270,276,282,288,294,300],{"slug":265,"cid":266,"name":267,"nameZh":267,"cas":268,"imgSvg":269},"785888974982877200","J-1358124-3","6-氨基-4-(3-氯-4-(...","848139-78-6","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F300\u002F848139-78-6.svg",{"slug":271,"cid":272,"name":273,"nameZh":273,"cas":274,"imgSvg":275},"785872802061226000","J-1310297-1","3-N,N-二甲氨基甲基丙烯酰氯盐酸盐","1055943-40-2","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F217\u002F1055943-40-2.svg",{"slug":277,"cid":278,"name":279,"nameZh":279,"cas":280,"imgSvg":281},"785896228914204700","J-1513950-1","[3-氯-4-(吡啶-2-甲氧...","524955-09-7","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F030\u002F524955-09-7.svg",{"slug":283,"cid":284,"name":285,"nameZh":285,"cas":286,"imgSvg":287},"785888391303532500","J-981811-5","二甲氨基乙醛缩二乙醇","3616-56-6","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F455\u002F3616-56-6.svg",{"slug":289,"cid":290,"name":291,"nameZh":291,"cas":292,"imgSvg":293},"785895140731392000","J-1507522-6","4-氯-3-氰基-7-乙氧基-...","214476-09-2","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F445\u002F214476-09-2.svg",{"slug":295,"cid":296,"name":297,"nameZh":297,"cas":298,"imgSvg":299},"785880696936730600","J-1083067-8","6-氨基-4-氯-7-乙氧基-...","848133-87-9","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F227\u002F848133-87-9.svg",{"slug":301,"cid":302,"name":303,"nameZh":303,"cas":304,"imgSvg":305},"785898012638449700","J-886588-1","2-氯-4-硝基酚","619-08-9","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F275\u002F619-08-9.svg",[],[],[309,312],{"key":310,"value":311},"危害码 (欧洲)","Xn",{"key":313,"value":314},"海关编码","29334900","2026-08-21T07:51:12.859463Z",false,[318,324,330,336,342,348,354,360,366,372,378,384],{"slug":319,"cid":320,"name":321,"nameZh":322,"cas":323},"785893207895445504","J-1064855-2","Polyquaternium-1","聚季铵盐-1","75345-27-6",{"slug":325,"cid":326,"name":327,"nameZh":328,"cas":329},"785893906318364672","J-36627-8","Disodium phthalocyanine","酞菁二钠","25476-27-1",{"slug":331,"cid":332,"name":333,"nameZh":334,"cas":335},"785892515826896896","J-32780-0","Copper PAN","铜-PAN络合物(CU-EDTA+PAN)","23299-85-6",{"slug":337,"cid":338,"name":339,"nameZh":340,"cas":341},"785875782072274944","J-10935-3","Sodium ionophore III","钠离子载体 III","81686-22-8",{"slug":343,"cid":344,"name":345,"nameZh":346,"cas":347},"785894942248538112","J-39715-9","Protoporphyrin IX","原卟啉","553-12-8",{"slug":349,"cid":350,"name":351,"nameZh":352,"cas":353},"785893395460526080","J-1929774-6","Aluminum phthalocyanine hydroxide","(SP-5-12)-羟基[29H,31H-酞菁根合-ΚN29,ΚN30,ΚN31,ΚN32]-铝","15554-15-1",{"slug":355,"cid":356,"name":357,"nameZh":358,"cas":359},"785881997733007360","J-21778-7","Manganese(II) phthalocyanine","锰(II)酞菁","14325-24-7",{"slug":361,"cid":362,"name":363,"nameZh":364,"cas":365},"785894115047903232","J-37219-0","Nickel, [29H,31H-phthalocyaninato(2-)-κN29,κN30,κN31,κN32]-, (SP-4-1)-","酞菁镍(II)","14055-02-8",{"slug":367,"cid":368,"name":369,"nameZh":370,"cas":371},"785896219460243456","J-1338606-6","Aluminum phthalocyanine cation","铝酞菁","47822-79-7",{"slug":373,"cid":374,"name":375,"nameZh":376,"cas":377},"785876270784188416","J-1099566-1","3-[(2,4-dinitrophenyl)diazenyl]-4-hydroxy-2,7-naphthalenedisulfonic acid disodium salt","硝氮黄","5423-07-4",{"slug":379,"cid":380,"name":381,"nameZh":382,"cas":383},"785929817445896192","J-494462-1","Etioporphyrin copper","初叶卟啉铜","54816-20-5",{"slug":385,"cid":386,"name":387,"nameZh":388,"cas":389},"785894492237467648","J-1310235-7","Mancopper","代森锰铜","53988-93-5",1794263003809,"zh-CN",[]]