[{"@context":"http:\/\/schema.org\/","@type":"BlogPosting","@id":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/5297#BlogPosting","mainEntityOfPage":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/5297","headline":"\u30d1\u30af\u30ea\u30c1\u30cb\u30d6 – Wikipedia","name":"\u30d1\u30af\u30ea\u30c1\u30cb\u30d6 – Wikipedia","description":"\u30d1\u30af\u30ea\u30c1\u30cb\u30d6 IUPAC\u547d\u540d\u6cd5\u306b\u3088\u308b\u7269\u8cea\u540d (16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene \u81e8\u5e8a\u30c7\u30fc\u30bf \u6cd5\u7684\u898f\u5236 \u6295\u4e0e\u65b9\u6cd5 \u7d4c\u53e3 \u8b58\u5225 ATC\u30b3\u30fc\u30c9 None PubChem CID: 46216796 ChemSpider 28518965 KEGG D11768 ChEMBL CHEMBL2035187 \u5225\u540d","datePublished":"2020-12-26","dateModified":"2020-12-26","author":{"@type":"Person","@id":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/author\/lordneo#Person","name":"lordneo","url":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/author\/lordneo","image":{"@type":"ImageObject","@id":"https:\/\/secure.gravatar.com\/avatar\/c9645c498c9701c88b89b8537773dd7c?s=96&d=mm&r=g","url":"https:\/\/secure.gravatar.com\/avatar\/c9645c498c9701c88b89b8537773dd7c?s=96&d=mm&r=g","height":96,"width":96}},"publisher":{"@type":"Organization","name":"Enzyklop\u00e4die","logo":{"@type":"ImageObject","@id":"https:\/\/wiki.edu.vn\/wiki4\/wp-content\/uploads\/2023\/08\/download.jpg","url":"https:\/\/wiki.edu.vn\/wiki4\/wp-content\/uploads\/2023\/08\/download.jpg","width":600,"height":60}},"image":{"@type":"ImageObject","@id":"https:\/\/upload.wikimedia.org\/wikipedia\/commons\/thumb\/1\/14\/Pacritinib_skeletal.svg\/230px-Pacritinib_skeletal.svg.png","url":"https:\/\/upload.wikimedia.org\/wikipedia\/commons\/thumb\/1\/14\/Pacritinib_skeletal.svg\/230px-Pacritinib_skeletal.svg.png","height":"168","width":"230"},"url":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/5297","about":["Wiki"],"wordCount":1947,"articleBody":"\u30d1\u30af\u30ea\u30c1\u30cb\u30d6IUPAC\u547d\u540d\u6cd5\u306b\u3088\u308b\u7269\u8cea\u540d(16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene\u81e8\u5e8a\u30c7\u30fc\u30bf\u6cd5\u7684\u898f\u5236\u6295\u4e0e\u65b9\u6cd5\u7d4c\u53e3\u8b58\u5225ATC\u30b3\u30fc\u30c9NonePubChemCID: 46216796ChemSpider28518965KEGGD11768 ChEMBLCHEMBL2035187\u5225\u540dSB1518\u5316\u5b66\u7684\u30c7\u30fc\u30bf\u5316\u5b66\u5f0fC28H32N4O3\u5206\u5b50\u91cf472.58 g\/molc1cc2cc(c1)-c3ccnc(n3)Nc4ccc(c(c4)COC\/C=C\/COC2)OCCN5CCCC5InChI=1S\/C28H32N4O3\/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26\/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)\/b4-3+Key:HWXVIOGONBBTBY-ONEGZZNKSA-N\u30c6\u30f3\u30d7\u30ec\u30fc\u30c8\u3092\u8868\u793a\u30d1\u30af\u30ea\u30c1\u30cb\u30d6 (Pacritinib, INN[1])\u306f\u3001\u9aa8\u9ac4\u7dda\u7dad\u75c7\u6cbb\u7642\u85ac\u3068\u3057\u3066\u958b\u767a\u304c\u9032\u3081\u3089\u308c\u3066\u3044\u308b \u74b0\u72b6\u30e4\u30cc\u30b9\u30ad\u30ca\u30fc\u30bc\u963b\u5bb3\u5264\u3067\u3042\u308b\u3002\u4e3b\u306b\u30e4\u30cc\u30b9\u30ad\u30ca\u30fc\u30bc2 (JAK2)\u3092\u963b\u5bb3\u3059\u308b\u3002\u81e8\u5e8a\u7b2cIII\u76f8\u8a66\u9a13\u304c2013\u5e74\u306b\u884c\u308f\u308c\u305f[2]\u3002  \u3053\u306e\u85ac\u306f\u30b7\u30f3\u30ac\u30dd\u30fc\u30eb\u306eS*\u30d0\u30a4\u30aaPte Ltd.\u3067\u767a\u898b\u3055\u308c\u305f\u3002JAK2\u963b\u5bb3\u6d3b\u6027\u306fJAK2\u91ce\u751f\u578b\u306b\u5bfe\u3057\u3066IC50 =23 nM\u3001JAK2 V617F\u5909\u7570\u306b\u5bfe\u3057\u3066 IC50=19 nM\u3067\u3042\u308a\u3001\u826f\u3044\u9078\u629e\u6027\u3092\u6301\u3063\u3066\u3044\u305f\u3002 JAK1  \u306b\u306fIC50=1280 nM\u3001JAK3\u306b\u306f IC50 =520nM\u3067\u3042\u3063\u305f[3][4]\u3002\u3053\u306e\u85ac\u5264\u306f Cell Therapeutics, Inc. (CTI)\u3068\u30d0\u30af\u30b9\u30bf\u30fc\u306b\u3088\u308a\u53d6\u5f97\u3055\u308c\u3001\u4ed6\u306eJAK\u963b\u5bb3\u5264\u3067\u306f\u8840\u5c0f\u677f\u6e1b\u5c11\u75c7\u3092\u304d\u305f\u3059\u9aa8\u9ac4\u7dda\u7dad\u75c7\u60a3\u8005\u306b\u5411\u3051\u958b\u767a\u304c\u9032\u3081\u3089\u308c\u3066\u3044\u308b[5]\u3002\u53c2\u8003\u8cc7\u6599[\u7de8\u96c6]^ \u201cInternational Nonproprietary Names for Pharmaceutical Substances (INN) List 104\u201d. WHO Drug Information 24 (4):  386. (2010). http:\/\/apps.who.int\/iris\/bitstream\/10665\/74579\/1\/24_4_2010_INN104.pdf.\u00a0^ \u201cJAK-Inhibitoren: Neue Wirkstoffe f\u00fcr viele Indikationen\u201d (German). Pharmazeutische Zeitung (21). (2013). http:\/\/www.pharmazeutische-zeitung.de\/index.php?id=46539.\u00a0^ William, A. D.; Lee, A. C. -H.; Blanchard, S. P.; Poulsen, A.; Teo, E. L.; Nagaraj, H.; Tan, E.; Chen, D. et al. (2011). \u201cDiscovery of the Macrocycle 11-(2-Pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2\/Fms-Like Tyrosine Kinase-3 (JAK2\/FLT3) Inhibitor for the Treatment of Myelofibrosis and Lymphoma\u201d. Journal of Medicinal Chemistry 54 (13):  4638\u201358. doi:10.1021\/jm200326p. PMID\u00a021604762.\u00a0^ Poulsen, A.; William, A.; Blanchard, S. P.; Lee, A.; Nagaraj, H.; Wang, H.; Teo, E.; Tan, E. et al. (2012). \u201cStructure-based design of oxygen-linked macrocyclic kinase inhibitors: Discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)\u201d. Journal of Computer-Aided Molecular Design 26 (4):  437\u201350. doi:10.1007\/s10822-012-9572-z. PMID\u00a022527961.\u00a0^ Baxter licenses cancer drug from CTI in $172m deal"},{"@context":"http:\/\/schema.org\/","@type":"BreadcrumbList","itemListElement":[{"@type":"ListItem","position":1,"item":{"@id":"https:\/\/wiki.edu.vn\/jp\/wiki6\/#breadcrumbitem","name":"Enzyklop\u00e4die"}},{"@type":"ListItem","position":2,"item":{"@id":"https:\/\/wiki.edu.vn\/jp\/wiki6\/archives\/5297#breadcrumbitem","name":"\u30d1\u30af\u30ea\u30c1\u30cb\u30d6 – Wikipedia"}}]}]