ProductDescription
XL184(Cabozantinib)isanoral,small-moleculeinhibitor,whichhaspotentactivitytowardVEGFR2(IC50=0.035nM)andMET(IC50=1.3nM),aswellasanumberofotherreceptortyrosinekinasesthathavealsobeenimplicatedintumorpathoBIOLOGy,includingRET,KIT,AXL,andFLT3[1].
Multiplereceptortyrosinekinases(RTKs)aresometimesactivatedinthesametumor.InhibitionofsingleRTKmayleadtocompensatorysignalingthatmaintainscellgrowth.Targetingmultiplekinasessimultaneouslymightovercomebothintrinsicandacquiredresistancetoantitumordrugs.XL184hasbeenshowntoinhibitphosphorylationofMETandVEGFR2,todisruptangiogenesisandcellularmigrationandinvasion,andtopromotetumorandendotheliacelldeath1.Inhibitionofc-MetwithXL184blocksself-renewalcapacityinpancreaticcancerstemcells(CSCs)[2].Inmousemodelsandpreclinicalstudies,XL184demonstratesrobustantiangiogenic,antitumor,andanti-invasiveeffects,dramaticallyalterstumorpathology,preventsthedevelopmentofmetastases,andreducestumorburden[1-3].
Technicalinformation:
ChemicalFormula: | C28H24FN3O5 | |
CAS#: | 849217-68-1 | |
MolecularWeight: | 501.51 | |
Purity: >98% | ||
Appearance: | White | |
ChemicalName: | N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | |
Solubility: | Upto22mMinDMSO | |
Synonyms: | XL184,XL-184,BMS-907351,BMS907351,Cabozantinib,Cometriq |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | YakesFM,etal.Cabozantinib(XL184),anovelMETandVEGFR2inhibitor,simultaneouslysuppressesmetastasis,angiogenesis,andtumorgrowth.MolCancerTher.2011.10(12):2298-308.PubmedID:21926191 |
2. | Herreros-VillanuevaM,etal.c-Metinpancreaticcancerstemcells:Therapeuticimplications.WorldJGastroenterol.2012.18(38):5321-3.PubmedID:23082047 |
3. | KurzrockR,etal.ActivityofXL184(Cabozantinib),anoraltyrosinekinaseinhibitor,inpatientswithmedullarythyroidcancer.JClinOncol.2011.29(19):2660-6.PubmedID:21606412 |
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MaggotsFasterThanScalpelinWoundDebridement
December19,2011—Maggotdebridementtherapy(MDT)appearstobemoreeffectiveforwounddebridementcomparedwithconventionaltherapy,butonlyat1week;afterthattime,anothertypeofdressingshouldbeused,newresearchsuggests.
KristinaOpletalovà,MD,fromtheDepartmentofDermatology,UniversityofCaen,France,andcolleaguespublishedonlineDecember19intheArchivesofDermatology.
MedicalmaggotswereapprovedbytheUSFoodandDrugAdmiNISTrationasamedicaldeviceforwounddebridementin2004.Accordingtotheresearchers,useofmaggotsintreatingwoundsisassociatedwitheffectivewounddebridement,antibacterialeffects,andstimulationofwoundhealing.
However,theypointout,"[r]elativelyfewclinicalstudieshavebeenconductedandtheresultsarenotclear,partlyowingtomethodologicassessmentproblems."
InthecurrentProspective,randomizedcontrolled,phase3clinicaltrial,theresearcherssoughttodeterminetheefficacyofbaggedlarvaeonwounddebridementincomparisonwithconventionaltreatment.
TheprimaryobjectivewastocomparethemeanpercentageofsloughinwoundstreatedwithMDTwiththatofconventionaltreatmentatday15.Thestudyincluded119patientswithanonhealing,sloughywoundthatwas40cm2orsmallerandlessthan2cmdeep.Patientsalsohadananklebrachialindexof0.8orhigher.
Treatmentwasadministeredduringa2-weekhospitalstay.Conventionaltreatmentconsistedofsurgicaldebridement3timesaweekwithascalpel,withuseoftopicalanesthesia.TheMDTwasadministeredusinganencloseddressing(Vitapad,BioMondeLaboratories)containing80sterilemaggots.Atdischarge,aconventionaldressingwasapplied,andpatientswerefollowed-upatday30.
DebridementbyMDTwassignificantlyfasterthansurgicaldebridementduringthefirstweekoftreatment,reachingthesamelevelthecontrolgroupreachedatday15.NobenefitforMDTcomparedwithconventionaltreatmentinhealingrateswasobserved.Atday8,54.5%intheMDTgroupvs66.5%inthecontrolgroup(P=.04)hadevidenceofsloughandwoundhealing.However,byday15,themeanpercentageofsloughwas55.4%intheMDTgroupand53.8%inthecontrolgroup(P=.78).
"AthoughMDTshowsnosignificantbenefitatday15comparedwithconventionaltreatment,debridementbyMDTissignificantlyfasterandoccursduringthefirstweekoftreatment,"theresearchersconclude."Becausethereisnobenefitincontinuingthetreatmentafter1week,anothertypeofdressingshouldbeusedafter2or3applicationsofMDT."
Painscoresweresimilarandmildinbothgroups,althoughincontrasttoconventionaltreatment,MDTwasperformedwithouttopicalanesthesia.
Accordingtotheresearchers,noneofthepatientswerereticentaboutundergoingMDT."[A]crawlingsensationonthewoundwasrarelyandalmostequallynotedinbothgroups,revealingthatthesensationwassubjective,"Dr.Opletalovàandcolleaguespointout.
TwoquestionsregardingMDTremainunanswered,theauthorsnote."Candebridementbeimprovedusingmoremaggotsperdressing?Ifso,wouldthesedressingsbemorepainful?Furtherstudiesareneededtoanswerthesequestions."
ThestudywassupportedbygrantsfromtheClinicalResearchHospitalProgramandfromtheFrenchSocietyofDermatology.Theauthorshavedisclosednorelevantfinancialrelationships.
1. 姜黄素是一个典型的HAT抑制剂。
2. 针对P300: 在大约10年前,Cole和他的同事设计出了一种p300/CBP抑制剂,发表在nature杂志上。
希望能帮到你,望采纳!
天然产物,大多都有颜色,
存在干扰,多数情况下需要做样品的阴性对照,
尽量能用荧光的方法,
之前我们做过,将两个试剂盒的方法合并后,做的,
效果还可以
支原体培养则是取样后在培养基上培养,看有多少支原体菌落会长出,是比较直观和可信的结果。
总体来讲,这两种检查手段可信度都较高,结合一起,不仅可以可靠的知道有无解脲支原体感染,还能知道感染是否严重。
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