Skip to main content

Quizartinib








Quizartinib


From Wikipedia, the free encyclopedia

Jump to navigation
Jump to search

























Quizartinib

Quizartinib.svg
Names

IUPAC name
1-(5-(tert-Butyl)isoxazol-3-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea

Other names
AC220

Identifiers

CAS Number



  • 950769-58-1 ☑Y


3D model (JSmol)


  • Interactive image


ChEBI


  • CHEBI:90217 ☒N


ChEMBL


  • ChEMBL576982 ☒N


ChemSpider


  • 24640357 ☒N


IUPHAR/BPS


  • 5658


KEGG

  • D09955


UNII


  • 7LA4O6Q0D3 ☑Y





Properties

Chemical formula


C29H32N6O4S

Molar mass
560.67 g·mol−1

Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).


☒N verify (what is ☑Y☒N ?)

Infobox references


Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor that is currently under development by Ambit Biosciences for the treatment of acute myeloid leukaemia. Its molecular target is FLT3, also known as CD135 which is a proto-oncogene.[1]


Flt3 mutations are among the most common mutations in acute myeloid leukaemia due to internal tandem duplication of Flt3. The presence of this mutation is a marker of adverse outcome.



Mechanism[edit]


Specifically, Quizartinib selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs).[citation needed]


Mutations cause constitutive action of Flt3 resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis.[citation needed]



Clinical trials[edit]


It reported good results in 2012 from a phase II clinical trial for refractory AML - particularly in patients who went on to have a stem cell transplant.[2]


As of 2017[update] it has completed 5 clinical trials and another 7 are active.[3]



References[edit]




  1. ^ Chao, Qi; Sprankle, Kelly G.; Grotzfeld, Robert M.; Lai, Andiliy G.; Carter, Todd A.; Velasco, Anne Marie; Gunawardane, Ruwanthi N.; Cramer, Merryl D.; Gardner, Michael F.; James, Joyce; Zarrinkar, Patrick P.; Patel, Hitesh K.; Bhagwat, Shripad S. (2009). "Identification of N-(5-tert-Butyl-isoxazol-3-yl)-N'-4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenylurea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor". Journal of Medicinal Chemistry. 52 (23): 7808–7816. doi:10.1021/jm9007533..mw-parser-output cite.citationfont-style:inherit.mw-parser-output qquotes:"""""""'""'".mw-parser-output code.cs1-codecolor:inherit;background:inherit;border:inherit;padding:inherit.mw-parser-output .cs1-lock-free abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/6/65/Lock-green.svg/9px-Lock-green.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .cs1-lock-limited a,.mw-parser-output .cs1-lock-registration abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/d/d6/Lock-gray-alt-2.svg/9px-Lock-gray-alt-2.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .cs1-lock-subscription abackground:url("//upload.wikimedia.org/wikipedia/commons/thumb/a/aa/Lock-red-alt-2.svg/9px-Lock-red-alt-2.svg.png")no-repeat;background-position:right .1em center.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registrationcolor:#555.mw-parser-output .cs1-subscription span,.mw-parser-output .cs1-registration spanborder-bottom:1px dotted;cursor:help.mw-parser-output .cs1-hidden-errordisplay:none;font-size:100%.mw-parser-output .cs1-visible-errorfont-size:100%.mw-parser-output .cs1-subscription,.mw-parser-output .cs1-registration,.mw-parser-output .cs1-formatfont-size:95%.mw-parser-output .cs1-kern-left,.mw-parser-output .cs1-kern-wl-leftpadding-left:0.2em.mw-parser-output .cs1-kern-right,.mw-parser-output .cs1-kern-wl-rightpadding-right:0.2em


  2. ^ Drug Tames Refractory AML. ASH Dec 2012


  3. ^ Quizartinib studies














Retrieved from "https://en.wikipedia.org/w/index.php?title=Quizartinib&oldid=784134561"





Navigation menu

























(window.RLQ=window.RLQ||).push(function()mw.config.set("wgPageParseReport":"limitreport":"cputime":"0.664","walltime":"0.819","ppvisitednodes":"value":6358,"limit":1000000,"ppgeneratednodes":"value":0,"limit":1500000,"postexpandincludesize":"value":223849,"limit":2097152,"templateargumentsize":"value":21653,"limit":2097152,"expansiondepth":"value":22,"limit":40,"expensivefunctioncount":"value":4,"limit":500,"unstrip-depth":"value":1,"limit":20,"unstrip-size":"value":4480,"limit":5000000,"entityaccesscount":"value":2,"limit":400,"timingprofile":["100.00% 608.504 1 -total"," 68.09% 414.304 1 Template:Chembox"," 38.39% 233.608 1 Template:Chembox_Identifiers"," 24.74% 150.530 3 Template:Chembox_headerbar"," 24.39% 148.400 9 Template:Trim"," 14.93% 90.823 10 Template:Main_other"," 14.69% 89.363 1 Template:Chembox_Properties"," 14.59% 88.767 1 Template:Reflist"," 13.13% 79.904 1 Template:Cite_journal"," 12.79% 77.819 1 Template:Chembox_parametercheck"],"scribunto":"limitreport-timeusage":"value":"0.229","limit":"10.000","limitreport-memusage":"value":4725237,"limit":52428800,"cachereport":"origin":"mw1271","timestamp":"20181010224750","ttl":1900800,"transientcontent":false);mw.config.set("wgBackendResponseTime":108,"wgHostname":"mw1320"););
-

Popular posts from this blog

The Dalles, Oregon

Image
The Dalles, Oregon From Wikipedia, the free encyclopedia Jump to navigation Jump to search This article is about the city in Oregon. For the nearby geological formation, see Celilo Falls. For other uses, see Dalles. Not to be confused with the town of Dallas, Oregon. City in Wasco County The Dalles City The Dalles and the Columbia River in November 2008 Flag Seal Motto(s):  "Cognito timor Vincit" (Latin), "Knowledge Conquers Fear" (English) Location in Oregon Coordinates: 45°36′4″N 121°10′58″W  /  45.60111°N 121.18278°W  / 45.60111; -121.18278 Coordinates: 45°36′4″N 121°10′58″W  /  45.60111°N 121.18278°W  / 45.60111; -121.18278 County Wasco County Incorporated 1857 Government  • Mayor Stephen Elliott Lawrence (D) [1] [2] Area [3]  • Total 6.61 sq mi (17.12...
Read more

眉山市

Image
Clash Royale CLAN TAG #URR8PPP   关于同名地方，参见：眉山郡、眉山县、眉山专区、眉山地区。 body.skin-minerva .mw-parser-output table.infobox captiontext-align:center 眉山市 三苏祠 简称 眉 地名出处 1.以峨眉山为名、2.城郊有山，分左右两峰，远望如眉，眉山由此而得名，此山现位于眉山电信“6501”单位内部、3.源于苏东坡。据说有人见他眉如山丘，智冠五...
Read more

清晰法令

Image
Clash Royale CLAN TAG #URR8PPP 本條目 部分链接不符合格式手冊規範 。跨語言链接及章節標題等處的链接可能需要清理。 ( 2015年12月11日 ) 請協助改善此條目。參見WP:LINKSTYLE、WP:MOSIW以了解細節。突出显示跨语言链接可以便于检查。 維基百科的法律內容只供參考， 並不能視作專業意見 。任何法律問題應諮詢相關司法管轄權...
Read more