{"id":82268,"date":"2019-04-08T00:00:50","date_gmt":"2019-04-11T06:59:16","guid":{"rendered":"http:\/\/www.05921.net\/index.php\/82268\/"},"modified":"2019-04-11T14:59:17","modified_gmt":"2019-04-11T06:59:17","slug":"f3057a0676","status":"publish","type":"post","link":"https:\/\/www.05921.net\/index.php\/82268\/","title":{"rendered":"\u4eceCrizotinib\u3001Ceritinib\u3001Alectinib\u548cBrigatinib\u63a2\u5bfb\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u836f\u7269\u7684\u53d1\u73b0\u4e4b\u65c5"},"content":{"rendered":"
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\"\u4eceCrizotinib\u3001Ceritinib\u3001Alectinib\u548cBrigatinib\u63a2\u5bfb\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u836f\u7269\u7684\u53d1\u73b0\u4e4b\u65c5\"<\/p>\n


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3\u3001\u827e\u4e50\u66ff\u5c3c\uff08Alectinib\uff09\u7684\u7814\u53d1\u4e4b\u65c5<\/span><\/section>\n
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Alectinib\u662f\u7531\u7f57\u6c0f\u516c\u53f8\u63a7\u80a1\u7684\u65e5\u672c\u4e2d\u5916\u5236\u836fChugai\u516c\u53f8\u7814\u53d1\u800c\u6210\u7684\u3002Chugai\u516c\u53f8\u901a\u8fc7\u9ad8\u901a\u91cf\u7b5b\u9009\u6280\u672f\u5bf9\u6fc0\u9176\u5316\u5408\u7269\u5e93\u8fdb\u884c\u7b5b\u9009\u53d1\u73b0\u5177\u6709\u56db\u73af\u6bcd\u6838\u7ed3\u6784\u7684\u884d\u751f\u7269C\u5177\u6709\u8f83\u597d\u7684\u5f00\u53d1\u524d\u666f\u3002\u6d3b\u6027\u7b5b\u9009\u53d1\u73b0\uff0c\u8be5\u884d\u751f\u7269\u5bf9\u95f4\u53d8\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\u5177\u6709\u8f83\u597d\u7684\u6291\u5236\u6d3b\u6027\uff0c\u800c\u5bf9c-Met\u51e0\u4e4e\u6ca1\u6709\u6291\u5236\u6d3b\u6027\uff0c\u8fd9\u8868\u660e\uff0c\u8be5\u884d\u751f\u5177\u6709\u8f83\u597d\u7684\u9009\u62e9\u6027\uff0c\u4e14\u6bd2\u526f\u4f5c\u7528\u8f83\u5c0f\u3002\u56e0\u6b64Chugai\u516c\u53f8\u901a\u8fc7\u7ed3\u6784\u4f18\u5316\u53d1\u73b0\uff0c\u5229\u7528\u5421\u54af\u73af\u66ff\u6362\u544b\u5583\u73af\u540e\uff0c\u5e76\u5728\u6bcd\u6838\u4e0a\u5f15\u5165\u6c30\u57fa\u5f97\u5230C1<\/span><\/sub>\uff0c\u6d3b\u6027\u6d4b\u5b9a\u53d1\u73b0\uff0cC1<\/span><\/sub>\u7684\u6d3b\u6027\u63d0\u9ad8\u4e86\u8fd1\u5343\u500d\uff1b\u968f\u540e\u518d\u5f15\u51654-\uff083-\u6c27\u6742\u73af\u4e01\u57fa\uff09\u54cc\u55ea\u7247\u6bb5\u540e\u5f97\u5177\u6709\u5168\u65b0\u9aa8\u67b6\u7684\u884d\u751f\u7269C2<\/span><\/sub><\/span>\uff0c\u4e14\u7814\u7a76\u53d1\u73b0\uff0c\u8be5\u884d\u751f\u7269\u7684\u4ee3\u8c22\u7a33\u5b9a\u6027\u5f97\u5230\u4e86\u76f8\u5e94\u7684\u63d0\u9ad8\u3002\u4e3a\u8fdb\u4e00\u6b65\u63d0\u9ad8C2<\/span><\/sub>\u7684\u9009\u62e9\u6027\uff0cChugai\u516c\u53f8\u5bf9\u95f4\u53d8\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\u8fdb\u884c\u4e86\u540c\u6e90\u6a21\u5efa\uff0c\u5bf9\u5316\u5408\u7269C2<\/span><\/sub>\u8fdb\u884c\u4e86\u5206\u5b50\u5bf9\u63a5\u5206\u6790\uff0c\u53d1\u73b0\u57289-\u4f4d\u5f15\u5165\u4e59\u57fa\u8fd9\u6837\u7684\u4e00\u4e2a\u4eb2\u8102\u6027\u53d6\u4ee3\u57fa\uff0c\u63d0\u9ad8\u4e86\u9009\u62e9\u6027\uff0c\u5f97\u5230\u4e86\u5316\u5408\u7269C3<\/span><\/sub>\u3002\u7ee7\u7eed\u5bf98-\u4f4d\u53d6\u4ee3\u57fa\u7684\u7ed3\u6784\u8fdb\u884c\u4f18\u5316\uff0c\u6700\u7ec8\u5f97\u5230\u4e86\u5177\u6709\u5f00\u53d1\u524d\u666f\u7684Alectinib\u3002<\/span><\/p>\n


<\/p>\n

\"\u4eceCrizotinib\u3001Ceritinib\u3001Alectinib\u548cBrigatinib\u63a2\u5bfb\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u836f\u7269\u7684\u53d1\u73b0\u4e4b\u65c5\"<\/p>\n


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4\u3001\u5e03\u683c\u66ff\u5c3c\uff08Brigatinib\uff09\u7684\u53d1\u73b0\u4e4b\u65c5<\/span><\/section>\n
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ARIAD\u5236\u836f\u516c\u53f8\u5bf9SRC\u6291\u5236\u5242AP23464\u4e2d\u7684\u4e8c\u7532\u57fa\u6c27\u5316\u78f7\u7247\u6bb5\u4ea7\u751f\u4e86\u6d53\u539a\u7684\u5174\u8da3\u3002\u5b83\u4eec\u57282\uff0c4-\u4e8c\u82b3\u6c28\u57fa\u5627\u5576\u6bcd\u6838\u4e2d\u5f15\u5165\u8be5\u7247\u6bb5\uff0c\u4ece\u800c\u8bbe\u8ba1\u5408\u6210\u4e86\u4e00\u7cfb\u5217\u542b\u78f7\u7684\u5627\u5576\u884d\u751f\u7269\uff0c\u6700\u7ec8\u5f97\u5230\u4e86\u5019\u9009\u836f\u7269AP26113\uff0c\u5373Brigatinib\u3002\u5728\u4f53\u5916\u95f4\u53d8\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\u7ee7\u53d1\u6027\u7a81\u53d8\u7ec6\u80de\u6a21\u578b\u4e2d\uff0cBrigatinib\u53ef\u9ad8\u6548\u6291\u523617\u4e2a\u95f4\u53d8\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\u7ee7\u53d1\u6027\u7a81\u53d8\uff0cIC50<\/span><\/sub>\u4ecb\u4e8e9nmol\/L\u548c184nmol\/L\u4e4b\u95f4\u3002<\/span><\/p>\n


<\/span><\/p>\n

\"\u4eceCrizotinib\u3001Ceritinib\u3001Alectinib\u548cBrigatinib\u63a2\u5bfb\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u836f\u7269\u7684\u53d1\u73b0\u4e4b\u65c5\"<\/p>\n


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\u968f\u7740\u5206\u5b50\u751f\u7269\u5b66\u548c\u9ad8\u901a\u91cf\u7b5b\u9009\u6280\u672f\u7684\u5feb\u901f\u53d1\u5c55\uff0c\u836f\u7269\u7814\u53d1\u4e5f\u9010\u6b65\u5411\u201c\u4e2a\u6027\u5316\u201d\u3001\u201c\u7cbe\u51c6\u5316\u201d\u8fc8\u8fdb\u3002\u4e0e\u5927\u591a\u6570\u836f\u7269\u4e00\u6837\uff0c\u6cbb\u7597\u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u7684\u836f\u7269\u4e5f\u4e0d\u53ef\u907f\u514d\u7684\u51fa\u73b0\u8010\u836f\u6027\u53ca\u5404\u79cd\u6bd2\u526f\u4f5c\u7528\uff0c\u800c\u79d1\u5b66\u5bb6\u4eec\u4e5f\u5728\u4e00\u6b65\u4e00\u6b65\u514b\u670d\u9669\u963b\uff0c\u671d\u7740\u8010\u836f\u6027\u4f4e\u4e14\u6bd2\u526f\u4f5c\u7528\u5c0f\u7684\u66f4\u9ad8\u6548\u836f\u7269\u8fc8\u8fdb\u3002<\/span><\/p>\n


<\/span><\/p>\n

\u53c2\u8003\u8d44\u6599<\/span><\/p>\n

[1] A Selectivesmall molecule inhibitor of c -Met kinase inhibits c -Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.<\/span><\/p>\n

[2] Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17 -tetrahydro -2H -8,4 -(metheno)pyrazolo [4,3 -h] [2,5,11] – benzoxadiaz-acyclotetradecine-3-carbonitrile(PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros on.<\/span><\/p>\n

[3] Discovery of entrectinib:a new 3 -aminoindazole as a potent anaplastic lymphoma kinase(ALK), c-ros oncogene 1 kinase (ROS1), and pan-tropomyosin receptor kinases (Pan-TRKs)inhibitor. <\/span><\/p>\n

[4] Chaptertwenty-five case history: XalkoriTM (Crizotinib), a potent and selective dual inhibitor of mesenchymal epithelial transition (MET) and anaplastic lymphoma kinase (ALK)for cancer treatment. <\/span><\/p>\n<\/p><\/div>\n","protected":false},"excerpt":{"rendered":"

\u8f6c\u81ea \u975e\u5c0f\u7ec6\u80de\u80ba\u764c\u662f\u5168\u7403\u6700\u5e38\u89c1\u7684\u6076\u6027\u80bf\u7624\u4e4b\u4e00\uff0c\u5bf9\u4eba\u7c7b\u8eab\u4f53\u5065\u5eb7\u9020\u6210\u6781\u5927\u7684\u5a01\u80c1\uff0c\u8fd1\u5e74\u6765\u5176\u53d1\u75c5\u7387\u548c\u75c5\u6b7b\u7387\u5747\u5448\u660e\u663e\u7684\u4e0a […]<\/p>\n","protected":false},"author":1,"featured_media":82269,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":[],"categories":[1],"tags":[],"_links":{"self":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/82268"}],"collection":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/comments?post=82268"}],"version-history":[{"count":1,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/82268\/revisions"}],"predecessor-version":[{"id":82273,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/posts\/82268\/revisions\/82273"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media\/82269"}],"wp:attachment":[{"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/media?parent=82268"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/categories?post=82268"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.05921.net\/index.php\/wp-json\/wp\/v2\/tags?post=82268"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}