AZD3229-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAZD3229Cat.No.:HY-112802CASNo.:2248003-60-1分?式:C??H??FN?O?分?量:479.51作?靶點(diǎn):c-Kit作?通路:ProteinTyrosineKinase/RTK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:40mg/mL(83.42mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0855mL10.4273mL20.8546mL5mM0.4171mL2.0855mL4.1709mL10mM0.2085mL1.0427mL2.0855mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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:4mg/mL(8.34mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:4mg/mL(8.34mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:4mg/mL(8.34mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性AZD3229?種有效的、?泛的突變型酪氨酸激酶受體(KIT)抑制劑，可?于開(kāi)發(fā)研究胃腸道間質(zhì)瘤。IC50&TargetKIT[1].體外研究AZD3229isapotent,pan-KITmutantinhibitorwithpotentsingledigitnMgrowthinhibitionagainstadiversepanelofmutantKITdrivenBa/F3celllines(GI50=1-50nM).AZD3229demonstratespotentsingledigitnMgrowthinhibitionacrossabroadcellpanel,withgoodmargintoKDR-driveneffects.SelectivityoverKDRcanberationalisedpredominantlybytheinteractionofwatermoleculeswiththeproteinandligandintheactivesiteanditskinomeselectivityissimilartothebestoftheapprovedGISTagents[1].REFERENCES[1].KettleJG,etal.DiscoveryofN-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1H-1,2,3-triazol-1-yl]acetamide(AZD3229),aPotentPan-KITMutantInhibitorfortheTreatmentofGastrointestinalStromalTumors.JMedMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T