ProductDescription
NVP-BGT226isanovelorallybioavailabledualPI3K/mTORinhibitor.ItselectivelyinhibitsPI3KandbothmTORcomplexesmTORC1andmTORC2,resultinginnearlycompletephosphorylation-inhibitionofP70S6and4E-BP1.
BGT226demonstratedexcellentcellularactivitiesininhibitingproliferations(IC50:7-30nM)ofmanytestedcelllines.Notably,cellsthatexpressPIK3CAmutationH1047Rarestillsensitivetothegrowth-inhibitionofBGT226.FlowcytometricanalysisshowsaccumulationofcellsintheG0-G1phasewithconcomitantlossintheS-phase.BGT226inducesapoptosisorautophagyofsomecancercellsatIC50lessthan25nM.Inanimalmodels,BGT226significantlydelays/inhibitstumorgrowthinadose-dependentmanner.BGT-226representsapotentialcandidateforcancertherapy.IthasenteredphaseI/IIclinicaltrialsfortreatmentofadvancedsolidtumors(includingbreastcancer)[1-4].
Technicalinformation:
ChemicalFormula: | C28H25F3N6O2.C4H4O4 | |
CAS#: | 1245537-68-1 | |
MolecularWeight: | 650.6 | |
Purity: | >98% | |
Appearance: | White | |
ChemicalName: | 8-(6-methoxypyridin-3-yl)-3-methyl-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1H-imidazo[4,5-c]quinolin-2(3H)-oneMaleicacid | |
Solubility: | Upto22mMinDMSO | |
Synonyms: | NVP-BGT226,BGT226 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | BaduraS,etal.PosterAbstracts.DifferentialSuppressiveEffectsofSelectivePI3KandmTORandDualPI3K/mTORC1/C2InhibitiononLong-TermCulturedPrimaryHumanAcuteLymphoblasticLeukemia(ALL)CellsImplicateaDistinctRoleofmTORC2https://ash.confex.com/ash/2010/webprogram/Paper33127.html |
2. | ChangKY,etal.Novelphosphoinositide3-kinase/mTORdualinhibitor,NVP-BGT226,displayspotentgrowth-inhibitoryactivityagainsthumanheadandneckcancercellsinvitroandinvivo.ClinCancerRes.2011.17(22):7116-26.PubmedID:21976531 |
3. | BaumannP,etal.SimultaneoustargetingofPI3KandmTORwithNVP-BGT226ishighlyeffectiveinmultiplemyeloma.AnticancerDrugs.2012.23(1):131-8.PubmedID:21959532 |
4. | http://clinicaltrials.gov/ct2/show/NCT00600275 |
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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。