{"id":15822,"date":"2018-03-07T13:02:29","date_gmt":"2018-03-07T05:02:29","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=15822"},"modified":"2022-07-20T17:19:34","modified_gmt":"2022-07-20T09:19:34","slug":"tpx-0005-alk%ef%bc%88%e9%96%93%e8%ae%8a%e6%80%a7%e6%b7%8b%e5%b7%b4%e7%98%a4%e6%bf%80%e9%85%b6%ef%bc%89%e6%8a%91%e5%88%b6%e5%8a%91-cas-2058227-19-1%e8%b2%a8%e8%99%9fb2027","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=15822","title":{"rendered":"TPX-0005 | ALK\uff08\u9593\u8b8a\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\uff09\u6291\u5236\u5291 CAS #2058227-19-1\u8ca8\u865fB2027"},"content":{"rendered":"

ALK\uff08\u9593\u8b8a\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\uff09\u6291\u5236\u5291\u7522\u54c1<\/span><\/strong><\/p>\n

\"ALK<\/p>\n

EGFR\u5c0f\u5206\u5b50\u6291\u5236\u5291\uff08\u8868\u76ae\u751f\u9577\u56e0\u5b50\u53d7\u9ad4\uff09\u5df2\u5ee3\u6cdb\u7528\u65bc\u80ba\u764c\u6cbb\u7642\u3002\u5df2\u7d93\u986f\u793a\u975e\u5c0f\u7d30\u80de\u80ba\u764c\uff08NSCLC\uff09\u7684\u4e00\u5c0f\u90e8\u5206\uff083-13\uff05\uff09\u5728ALK\uff08\u9593\u8b8a\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\uff09\u57fa\u56e0\u4e2d\u5177\u6709\u91cd\u6392\u3002\u5728\u904e\u53bb\u5e7e\u5e74\u4e2d\uff0c\u8207\u5e38\u898f\u5316\u7642\u76f8\u6bd4\uff0cALK\u6291\u5236\u5291\u5728ALK\u967d\u6027\u975e\u5c0f\u7d30\u80de\u80ba\u764c\u7684\u6cbb\u7642\u4e2d\u986f\u793a\u51fa\u986f\u8457\u7684\u76ca\u8655\u3002\u651c\u5e36ALK\u67d3\u8272\u9ad4\u91cd\u6392\u7684\u665a\u671f\u975e\u5c0f\u7d30\u80de\u80ba\u764c\u60a3\u8005\u7684\u6cbb\u7642\u5df2\u7d93\u7531Crizotinib\uff08\u4e00\u7a2e\u916a\u6c28\u9178\u6fc0\u9176ALK\uff0cROS1\u548cMET\u7684\u5c0f\u5206\u5b50\u6291\u88fd\u5291\uff09\u7684\u767c\u5c55\u5e36\u4f86\u4e86\u9769\u547d\u6027\u7684\u8b8a\u5316\u3002\u7136\u800c\uff0c\u4f7f\u7528\u514b\u5511\u66ff\u5c3c\u6cbb\u7642NSCLC\u7684\u4e2d\u6a1e\u795e\u7d93\u7cfb\u7d71\u6709\u9650\u7684\u7121\u9032\u5c55\u751f\u5b58\u671f\uff08PFS\uff09\u548c\u9032\u5c55\u901f\u7387\u5c0e\u81f4\u4e86\u7b2c\u4e8c\u4ee3ALK\u6291\u5236\u5291\u5982Ceritinib\uff08Zykadia\uff09\u548cAlectinib\uff08Alecensa\uff09\u7684\u767c\u5c55\u53ef\u4ee5\u6291\u5236\u9a45\u52d5\u514b\u91cc\u5511\u66ff\u5c3c\u8010\u85e5\u7684\u5927\u591a\u6578\u81e8\u5e8a\u89c0\u5bdf\u5230\u7684ALK\u7a81\u8b8a\u3002\u5e7e\u7a2e\u65b0\u7684\u916a\u6c28\u9178\u6fc0\u9176\u6291\u5236\u5291\uff08TKIs\uff09\u8655\u65bcALK\u967d\u6027\u764c\u75c7\u7684\u81e8\u5e8a\u767c\u5c55\u7684\u4e0d\u540c\u968e\u6bb5\u3002\u9019\u4e9b\u85e5\u7269\u4e2d\u7684\u8a31\u591a\u5728CNS\u548c\u5c0d\u514b\u5511\u66ff\u5c3c\u6709\u6297\u6027\u7684\u764c\u75c7\u4e2d\u90fd\u5177\u6709\u6d3b\u6027\u3002<\/p>\n

TPX-0005 <\/strong>| <\/strong>CAS #<\/strong>2058227-19-1\u8ca8\u865f<\/strong>B2027<\/a><\/span><\/p>\n

A selective ALK inhibitor<\/em><\/strong><\/p>\n

\u7522\u54c1<\/strong>\u63cf\u8ff0\uff1a<\/strong>TPX-0005\u662f\u4e00\u7a2e\u6709\u6548\u7684ALK\u6291\u5236\u5291\u3002 \u5b83\u6291\u5236WT ALK\uff08IC 50 1.01nM\uff09\u548c\u5305\u62ecALK G1202R\uff08IC 50 = 1.26nM\uff09\u548cALK L1196M\uff08IC 50 = 1.08nM\uff09\u7684\u7a81\u8b8a\u3002 \u6b64\u5916\uff0cTPX-0005\u5728ALK WT\u548cALK G1202R\u7570\u7a2e\u79fb\u690d\u7269\u4e2d\u6709\u6548\u6291\u5236\u9ad4\u5167\u816b\u7624\u751f\u9577\u3002 TPX-0005\u4e5f\u662f\u4e00\u7a2e\u6709\u6548\u7684SRC\u6291\u5236\u5291\uff08IC 50 = 5.3nM\uff09\u3002<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Alternate Name<\/strong><\/td>\n(13E,14E,3R,6S)-45-fluoro-3,6-dimethyl-5-oxa-2,8-diaza-1(5,3)-pyrazolo[1,5-a]pyrimidina-4(1,2)-benzenacyclononaphan-9-one<\/td>\n<\/tr>\n
Appearance<\/strong><\/td>\nCrystalline solid<\/td>\n<\/tr>\n
CAS #<\/strong><\/td>\n2058227-19-1<\/td>\n<\/tr>\n
Molecular Formula<\/strong><\/td>\nC\u2081\u2088H\u2081\u2088FN\u2085O\u2082<\/td>\n<\/tr>\n
Molecular Weight<\/strong><\/td>\n355.37<\/td>\n<\/tr>\n
Purity<\/strong><\/td>\n\u226598% by HPLC<\/td>\n<\/tr>\n
Solubility<\/strong><\/td>\nDMSO<\/td>\n<\/tr>\n
SMILES<\/strong><\/td>\nCC1CNC(=O)C2=CNN3C2=NC(=NC(C4=C(O1)C=CC(=C4)F)C)C=C3<\/td>\n<\/tr>\n
InChi<\/strong><\/td>\nInChI=1S\/C18H18FN5O2\/c1-10-8-20-18(25)14-9-21-24-6-5-16(23-17(14)24)22-11(2)13-7-12(19)3-4-15(13)26-10\/h3-7,9-11,21H,8H2,1-2H3,(H,20,25)\/t10-,11+\/m0\/s1<\/td>\n<\/tr>\n
InChi Key<\/strong><\/td>\nRZNJKDGJGCKKNC-WDEREUQCSA-N<\/td>\n<\/tr>\n
PubChem CID<\/strong><\/td>\n118265583<\/td>\n<\/tr>\n
Handling<\/strong><\/td>\nProtect from air and light<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

\"\u76f8\u95dc\u8a66\u5291\"<\/strong>\u00a0A 83-01\u6291\u5236\u5291\u00a0<\/a>\u00a0|\u00a0\u00a0TPX-0005\u6291\u5236\u5291\u00a0<\/a>\u00a0|\u00a0NVP-TAE684<\/a>\u6291\u5236\u5291\u00a0|\u00a0Belizatinib (TSR-011)<\/a>\u6291\u5236\u5291<\/span><\/strong><\/p>\n

\u00a0<\/strong><\/p>\n","protected":false},"excerpt":{"rendered":"

ALK\uff08\u9593\u8b8a\u6027\u6dcb\u5df4\u7624\u6fc0\u9176\uff09\u6291\u5236\u5291\u7522\u54c1 EGFR\u5c0f\u5206\u5b50\u6291\u5236\u5291\uff08\u8868\u76ae\u751f\u9577\u56e0\u5b50\u53d7\u9ad4\uff09\u5df2\u5ee3\u6cdb\u7528\u65bc\u80ba\u764c\u6cbb\u7642\u3002\u5df2\u7d93\u986f\u793a\u975e\u5c0f […]<\/p>\n","protected":false},"author":3,"featured_media":15823,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[478,486],"tags":[2870],"_links":{"self":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/15822"}],"collection":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=15822"}],"version-history":[{"count":2,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/15822\/revisions"}],"predecessor-version":[{"id":15845,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/15822\/revisions\/15845"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/15823"}],"wp:attachment":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=15822"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=15822"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=15822"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}