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靶向药原料药厂家,PF06463922原料药价格

发布时间 2016-08-12 收藏 分享
价格 10.00
区域 湖北省 - 武汉市
来源 湖北帝鑫化工有限公司销售部

详情描述:

靶向药原料药厂家,PF06463922原料药价格PF06463922产品名称: PF06463922英文名:PF 06463922别名: (10R)-7-Amino-12-fluoro-10,15,16,17-tetrahydro-2,10,16-trimethyl-15-oxo-2H-4,8-methenopyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile产品名称: PF 06463922CAS 号:1454846-35-5, PF 06463922分子式: C21H19FN6O2分子量: 406.41产品简述           PF-06463922 is a novel, orally available, CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively.详细说明          PF-06463922 demonstrates significant cell activity against ALK and a large set of ALK clinical mutations with IC50 ranging from 0.2 nM-77 nM. PF-06463922 exhibited subnanomolar cellular potency against oncogenic ROS1 fusions and inhibited the crizotinib-refractory ROS1(G2032R) mutation and the ROS1(G2026M) gatekeeper mutation. Compared with crizotinib and the second-generation ALK/ROS1 inhibitors ceritinib and alectinib, PF-06463922 showed significantly improved inhibitory activity against ROS1 kinase. in vivo: PF-06463922 showed marked antitumor activity in tumor models expressing FIG-ROS1, CD74-ROS1, and the CD74-ROS1(G2032R) mutation. Furthermore, PF-06463922 demonstrated antitumor activity in a genetically engineered mouse model of FIG-ROS1 glioblastoma.   PF06463622是克唑替尼2代产品,在总的ALK抑制剂中划分到第3代。现在ALK的用药方案为克唑替尼--AP26113,CH5424802,LDK378--PF06463922。3922的作用力为克唑替尼的40倍,是AP26113的6倍。3922能抑制克唑替尼耐药之后的9种突变,AP只能抑制剂2种,CH能抑制3种,LDK378能抑制4种,但AP和LDK378是姐妹药,结构、作用机理基本相同。3922采用全新的大环结构,作用机理和效果大幅增加。3922还可以抑制ros1靶点,其作用力是alk的3倍,是目前ros1的2代药。3922应该是目前***广谱及活性的ALK/ROS抑制剂。1,公司对公账户和企业法人账户统一汇款,杜绝私人买卖行为,让客户放心。2,客户如何购买,有何疑问,请咨询联系方式 :15623615940    027-51904722    qq:28263329983,湖北帝鑫化工制造有限公司秉承“专业    诚信    信赖”的经营理念,以“质量,顾客满意”作为我们质量政策。

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