NAZ2329-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENAZ2329Cat.No.:HY-103693分?式:C??H??F?NO?S?分?量:501.56作?靶點(diǎn):Phosphatase作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(199.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9938mL9.9689mL19.9378mL5mM0.3988mL1.9938mL3.9876mL10mM0.1994mL0.9969mL1.9938mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.98mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.98mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.98mM);ClearsolutionBIOLOGICALACTIVITY?物活性NAZ2329受體型蛋?質(zhì)酪氨酸磷酸酶(RPTPs)R5亞家族的第?個(gè)細(xì)胞可滲透抑制劑，相對(duì)于其他PTPs，它變構(gòu)且優(yōu)先抑制PTPRZ(hPTPRZ1的IC50=7.5μM)和PTPRG(hPTPRGIC50=4.8μM)。NAZ2329與PTPRZ的D1結(jié)構(gòu)域結(jié)合，相對(duì)于PTPRZ整個(gè)(D1+D2)?段，其更有效地抑制PTPRZ1-D1?段，其IC50為1.1μM。NAZ2329可有效抑制膠質(zhì)母細(xì)胞瘤細(xì)胞的腫瘤?長并抑制?細(xì)胞樣特性。IC50&TargetIC50:7.5μM(PTPRZ),4.8μM(PTPRG),35.7μM(PTPRA),56.7μM(PTPRM),23.7μM(PTPRS),35.4μM(PTPRB),15.2μM(PTPN6),14.5μM(PTPN1)[1]體外研究NAZ2329(0-25μM;48hours)dose-dependentlyinhibitscellproliferationandmigrationinallcelllines(ratglioblastomacellsbearingC6cloneandhumanU251glioblastomacells)[1].NAZ2329(25μM;0-90min)obviouslypromotesthephosphorylationlevelofpaxillinatTyr-118site,leadingtoinhibitionforPTPRsubstrate[1].CellProliferationAssay[1]CellLine:RatglioblastomacellsbearingC6clone,humanU251glioblastomacellsConcentration:0μM,6.3μM,12.5μM,25μMIncubationTime:48hoursResult:Exertedinhibitionincellproliferationandmigrationinadose-dependentmanner.WesternBlotAnalysis[1]CellLine:RatglioblastomacellsbearingC6cloneConcentration:25μMIncubationTime:0min,15min,30min,60min,90minResult:PromotedthephosphorylationlevelofpaxillinatTyr-118site.體內(nèi)研究NAZ2329(22.5mg/kg;intraperitonealinjection;twiceperweek;40days)alonehasamoderateinhibitoryeffect.However,thecombinationofTemozolomideandNAZ2329exertsasignificantlyincreasedinhibitionoftumorgrowthcomparedwiththecontrolgroup,theNAZ2329monotherapygroupandtheTemozolomidemonotherapygroup[1].AnimalModel:FemaleBALB/c-nu/numiceaged4week-oldbearingparentalorPtprz-knockdownC6cells[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:22.5?mg/kg;Temozolomide(TMZ,50?mg/kg)Administration:Intraperitonealinjection;twiceperweek;40daysResult:ThecombinationofNAZ2329andTMZsignificantlydelayedtumorgrowthcomparedtoNAZ2329orTMZalone.REFERENCES[1].AkihiroFujikawa,etal.TargetingPTPRZinhibitsstemcell-likepropertiesandtumorigenicityinglioblastomacells.SciRep.2017Jul17;7(1):5609.McePdfHeightCaution:Producthasnotbeenfull