Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBPR1K871Cat.No.:HY-100865CASNo.:2443767-35-7Synonyms:DBPR114分?式:C??H??ClN?O?S分?量:526.05作?靶點(diǎn):FLT3作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(237.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9010mL9.5048mL19.0096mL5mM0.3802mL1.9010mL3.8019mL10mM0.1901mL0.9505mL1.9010mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(3.95mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.95mM);ClearsolutionBIOLOGICALACTIVITY?物活性BPR1K871(DBPR114)?種?效選擇性的FLT3/AURKA雙重抑制劑，對FLT3和AURKA作?的IC50值分別為19nM和22nM。BPR1K871可?于癌癥的研究[1]。IC50&TargetIC50:19nM(FLT3),22nM(AURKA)[1]體外研究BPR1K871showspotentanti-proliferativeactivitiesinMOLM-13andMV4-11AMLcellswithanEC50of~5nM[1].體內(nèi)研究BPR1K871isamulti-kinaseinhibitorforthetreatmentofacutemyeloidleukemia(AML)andsolidtumors[1].REFERENCES[1].HsuYC,etal.DiscoveryofBPR1K871,aquinazolinebased,multi-kinaseinhibitorforthetreatmentofAMLandsolidtumors:Rationaldesign,synthesis,invitroandinvivoevaluation.2016Dec27;7(52):86239–86256.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;