CAS: 1058137-23-7; 6-((7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-yl)Oxy)-N-Methyl-1-Naphthamide
该化合物是一个小分子抑制器,主要以其在针对特定受体强力强抗体,特别是涉及癌症信号路径的受体强力激素运动器的作用而闻名,其特点是能够抑制纤维增殖因子受体(FGFRs)和血盘增殖因子受体(PDGFRs)的活动,这些受体与肿瘤生长和血管生长有关.卢西塔尼布因其在各种癌症(包括乳腺癌和肺癌)中的治疗应用潜力而受到调查,特别是在有特定基因突变或改变的情况下.该化合物通常通过口试进行临床试验,以评估其功效和安全性能.其化学结构包括多种功能组,有助于其生物活动和药用基因特性.与许多有针对性的疗法一样,卢西塔尼布的效力可能因肿瘤的分子特性和特定生物标志的存在而不同.
- 英文名称6-((7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-yl)Oxy)-N-Methyl-1-Naphthamide
- 中文名称6-[[7-[(1-氨基环丙基)甲氧基]-6-甲氧基-4-喹啉基]氧基]-N-甲基-1-萘甲酰胺
- IUPAC名称6-((7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-N-methyl-1-naphthamide
- 其它别名1,13-Dimethyl-10-(3-Methyl-2-Butenyl)-(1R,9R,13R)-10-Azatricyclo[7.3.1.02,7]Trideca-2(7),3,5-Trien-4-Ol(Pentazocine); Lucitanib [who-Dd]; Pentobarbitone (Van); 6-((7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-yl)Oxy)-N-Methyl-1-Naphthamide; Amy
- CAS编号1058137-23-7
- MFCD编号:MFCD20527751
- FDA UNII编号:PP449XA4BH
- 分子式:C26H25N3O4分子量:443.5
- 产品CID: 99080
- 同类组份化合物CAS1058137-23-7 (free base)2108875-91-6 (HCl)
- 产品分类生物化工 → 抑制剂 → 蛋白酪氨酸激酶
物理性质
- 沸点696.5±50.0 °C(预测)
- 密度1.285±0.06 g/cm3(预测)
- pKa:14.65±0.46(预测)
- PSA:99.19
- LogP:5.6937
- 溶解性Soluble In DMSO
- 外观形态白色至黄色粉末
- 储存条件储存在 -20°C
- 产品应用该化合物是VEGFR和FGFFR的双重抑制剂,表明VEGBFR1,VEFFFI2,V EGFRI2, VEG FFR3,FG FR1和FFGR2的强大和选择性抑制作用,IC50值分别为7纳米M,25纳米米,10纳米M,17.5纳米M和82.5纳米M;它也以5纳米的IC50来抑制CSF-1R;它有效抑制VE GF-和BFGGF-刺激的HUVEC扩散(分别为IC50=40和50纳米),并显示出强烈的抗血管诱变活动,7天完全抑制BFFFFF引起的血管在活性20毫克/千克口服20毫克的BGFFFR2, LUITANI B显示多种X-光谱抗脉冲效果,在多种XGRAFT模型中,包括HT29结肠癌,A2780卵癌, AA498,SNS12K1和RXF393 全面诱变性肿瘤,以及明显的肿瘤病状瘤.
上下游产品
benzyl 1-((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)methyl)cyclo-propylcarbamate 6-(7-(benzyloxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide 6-hydroxy-1-naphthoic acid 6-hydroxy-N-methyl-1-naphthalenecarboxamide合成工艺路线路线简述
📜4-Methoxybenzyl 1-((6-Methoxy-4-(5-(Methylcarbamoyl)-Naphthalen-2-Yloxy)-Quinolin-7-Yloxy)Methyl)Cyclopropylcarbamate 以95.9的收率获得6-[[7-[(1-氨基环丙基)甲氧基]-6-甲氧基-4-喹啉基]氧基]-N-甲基-1-萘甲酰胺
参考文献:Process For Preparing The Anti-Tumor Agent 6-(7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-Yloxy)-N-Methyl-1-Naphthamide And Its Crystalline
标题:Process For Preparing The Anti-Tumor Agent 6-(7-((1-Aminocyclopropyl)Methoxy)-6-Methoxyquinolin-4-Yloxy)-N-Methyl-1-Naphthamide And Its Crystalline
摘要:本发明涉及一种通过在稀释或弱酸性条件下去保护取代苄基1-((6-甲氧基-4-(5-(甲基氨基)Naphthalen-2-Yloxy)Quinolin-7-Yloxy)-甲基)Cyc-Lopropylcarbamate (公式i)合成6-(7-((1-氨基环丙基)-甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘酰胺(Al3810)的新工艺.同时,还制备了一种稳定的晶体形态6-(7-((1-氨基环丙基)-甲氧基)-6-甲氧基喹啉-4-氧基)-N-甲基-1-萘酰胺.
专利信息
专利号:JP-6061158-B2
优先权日:2009-03-16
标题:Synthesis intermediate of 6- (7-((1-aminocyclopropyl) methoxy) -6-methoxyquinolin-4-yloxy) -N-methyl-1-naphthamide, or a pharmaceutically acceptable salt thereof, and its use
专利号:JP-2015180665-A
优先权日:2009-03-16
标 题:Synthesis intermediate of 6- (7-((1-aminocyclopropyl) methoxy) -6-methoxyquinolin-4-yloxy) -N-methyl-1-naphthamide, or a pharmaceutically acceptable salt thereof, and its use
专利号:IT-MI20090397-A1
优先权日:2009-03-16
标 题 :PROCEDURE FOR THE PREPARATION OF 6- (7 - ((1-AMINOCYCLOPROPYL) METHOSSI) -6-METOSSICHINOLIN-4-ILOSSI) -N-METHYL-1-NAFTAMIDE AND ITS INTERMEDIATES OF SYNTHESIS
专利号:PT-2641897-T
优先权日:2009-03-16
标题 :A PROCESS FOR THE PREPARATION OF 6- (7 - ((1-AMINOCYCLOPROPYL) METHOXY) -6-METHOXYQUINOLIN-4-YLOXY) -N-METHYL-1-NAFTAMIDE AND ITS SYNTHESIS INTERMEDIATES
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: Colzani M, Noberini R, Romanenghi M, Colella G, Pasi M, Fancelli D, Varasi M, Minucci S, Bonaldi T. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. doi: 10.1074/mcp.M113.034173. Epub 2014 Apr 2.
2: Zangarini M, Ceriani L, Bello E, Damia G, Cereda R, Camboni MG, Zucchetti M. HPLC-MS/MS method for quantitative determination of the novel dual inhibitor of FGF and VEGF receptors E-3810 in tumor tissues from xenograft mice and human biopsies. J Mass Spectrom. 2014 Jan;49(1):19-26. doi: 10.1002/jms.3305. doi: 10.1158/1535-7163.MCT-12-0275-T. Epub 2012 Dec 27. doi: 10.1111/j.1582-4934.2012.01601.x. doi: 10.1002/jms.1985. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. Japanese.
合成参考文献
参考文献:10.1007/s11864-019-0667-9
摘要:Gerratana L, Davis AA, Shah AN, Lin C, Corvaja C, Cristofanilli M. Emerging Role of Genomics and Cell-Free DNA in Breast Cancer. Curr Treat Options Oncol. 2019 Jun 29;20(8):68. doi: 10.1007/s11864-019-0667-9.
参考文献:10.1007/bf02100139
摘要:Xu G, Sumi S, Koike M, Tanigawa K, Nio Y, Tamura K. Role of endogenous hypergastrinemia in regenerating endocrine pancreas after partial pancreatectomy. Digestive Diseases and Sciences. 1996 Dec;41(12):2433–9. doi: 10.1007/bf02100139.
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