中文名称鲁索利替尼磷酸盐中文同义词卢索替尼磷酸盐;(3R)-3-环戊基-3-4-[(7H吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑基]丙腈磷酸;磷酸鲁索利替尼;磷酸卢索替尼;鲁索替尼磷酸盐;(BETAR)-BETA-环戊基-4-(7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-丙腈磷酸盐(鲁索利替尼);(BETAR)-BETA-环戊基-4-(7H-吡咯并[2,3-D]嘧啶-4-基)-1H-吡唑-1-丙腈磷酸盐(鲁索利替尼磷酸盐);鲁索利替尼磷酸盐英文名称Ruxolitinibphosphate英文同义词(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrilephosphate;INCB018424;Ruxolitinib,PhosphateSalt;Ruxolitinib,Phosphate;(βR)-β-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazole-1-propanenitrilePhosphate;INCB018424;INCB-018424;INCB018424;(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrilephosphoricacid;Ruxolitinib(INCB-18424)phosphateCAS号1092939-17-7分子式C17H21N6O4P分子量404.37EINECS号相关类别抗肿瘤药物;小分子抑制剂;医药原料药;医药原料;小分子抑制剂,天然产物;其它中间体;化工原料;原料;标准品;化学试剂;Intracellularsignaling.;Inhibitors;Antineoplastic;APIMol文件1092939-17-7.mol结构式鲁索利替尼磷酸盐性质熔点186-190°C储存条件Refrigerator溶解度可溶于DMSO(少许)、甲醇(少许)形态固体颜色白色至类白色InChIInChI=1/C17H18N6.H3O4P/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/s3InChIKeyJFMWPOCYMYGEDM-AVAJOTNLNA-NSMILESP(O)(O)(O)=O.[C@@H](C1CCCC1)(N1N=CC(C2N=CN=C3NC=CC=23)=C1)CC#N|&1:5,Chemicalbookr|鲁索利替尼磷酸盐用途与合成方法简介Ruxolitinibphosphate是一种有效的JAK1/2抑制剂,IC50分别为3.3nM/2.8nM,比JAK3选择性高130倍。体外研究Ruxolitinib(INCB018424)有效且选择性地抑制JAK2V617F介导的信号传导和增殖。Ruxolitinib抑制HEL细胞的生长,EC50为186nM。Ruxolitinib显着增加Ba/F3-EpoR-JAK2V617F细胞系统的凋亡,并抑制原发性MPN患者样本中的造血祖细胞增殖。体内研究Ruxolitinib(180mg/kg,po)可降低接种JAK2V617F表达细胞的小鼠的肿瘤负荷,而不会引起贫血或淋巴细胞减少。生物活性RuxolitinibPhosphate(INCB018424,INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib是第一个应用于临床的,有效的,选择性JAK1/2抑制剂,在无细胞试验中IC50为3.3nM/2.8nM。作用于JAK1,JAK2与作用于JAK3相比,选择性高130多倍。Ruxolitinib通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib可诱导自噬并增强细胞凋亡。靶点TargetValueJAK2(Cell-freeassay)2.8nMJAK1(Cell-freeassay)3.3nM用途一种有效的JAK1/2抑制剂,IC50分别为3.3nM/2.8nM,比JAK3选择性高130倍。RuxolitinibisanorallybioavailableJanus-associatedkinase(JAK)inhibitorwithpotentialantineoplasticandimmunomodulatingactivities.RuxolitinibspecificallybindstoandinhibitsproteintyrosinekinasesJAK1and2,whichmayleadtoareductionininflammationandaninhibitionofcellularproliferation.TheJAK-STAT(signaltransducerandactivatoroftranscription)pathwayplaysakeyroleinthesignalingofmanycytokinesandgrowthfactorsandisinvolvedincellularproliferation,growth,hematopoiesis,andtheimmuneresponse;JAKkinasesmaybeupregulatedininflammatorydiseases,myeloproliferativedisorders,andvariousmalignancies. |