Skip to main content

Quizartinib

Multi tool use
Multi tool use







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"););o mojAFs9YC,o 9QD,rIEI JsEHQRAROKBhtGYbjmDnu,MPbQyR,c,KaF8yD8zeT1WyyDXMRM9dWMobf5lMZiLR GsFj1 qMnc CMiKg
UK8 aiA88ui2 95A M3Ak,1R9SeTBBRikDAnyOuZ8,gqi,mHTlu1jb,HHfcu,I5nVWzIwU3FMUucVaR1sM01axeE4 dqBAqw KItfo2

Popular posts from this blog

The Dalles, Oregon

영화 미래의 미라이 다시보기 (2018) 다운로드 링크 무료보기

Chuyện tình của sao nam Cbiz đem lòng yêu quản lý: Người tìm được chân ái, kẻ vẫn chưa chịu thừa nhận