Sovleplenib-HMPL-523-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESovleplenibCat.No.:HY-145598CASNo.:1415792-84-5Synonyms:HMPL-523分?式:C??H??N?O?S分?量:482.6作?靶點:Syk作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:25mg/mL(51.80mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0721mL10.3605mL20.7211mL5mM0.4144mL2.0721mL4.1442mL10mM0.2072mL1.0361mL2.0721mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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(4.31mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.31mM);ClearsolutionBIOLOGICALACTIVITY?物活性Sovleplenib(HMPL-523)?種?效的、可?服的選擇性SYK抑制劑，IC50為25nM。具有抗腫瘤活性。Sovleplenib可?于免疫性??板減少癥（ITP）的研究[1]。IC50&TargetSYK[1]體外研究Sovleplenib(HMPL-523)inhibitsSYK,FLT3,KDR,LYN,FGFR2,andAURAwithIC50sof0.025,0.063,0.390,0.921,3.214,3.969μM,respectively[1].Sovleplenib(HMPL-523)blocksphosphorylationofBLNK,downstreamproteinofSyk,inhumanmantlecelllineREC-1andhumanplasmacelllineARH-7777withIC50sof0.105μMand0.173μM,respectively[2].SovleplenibalsoinhibitscellviabilityofBa/F3Tel-SykwiththeIC50of0.033μM[2].SovleplenibalsoincreasestheapoptoticrateofREC-1cells[2].SovleplenibshowsthesynergisticactivitiesonkillinghumandiffusedlargeBcelllymphoma(DLBCL)incombinationwithotherdrugssuchasBTKinhibitor,PI3KδinhibitorsandBcl2familyinhibitor[2].體內(nèi)研究Sovleplenib(HMPL-523)showsanti-tumoractivityinvivo.Sovleplenib(100mg/kg)inhibitstumorgrowthinREC-1subcutaneousxenograftmodel[1].Sovleplenib(HMPL-523;100mg/kg;dailyoraladministration)showspotentanti-tumoractivityinBcelllymphomaREC-1(TGI:59%)inSykdependentxenograftmodels[2].AnimalModel:Balb/cnudemicebearingsubcutaneouslyimplantedREC-1cellsorintravenouslyinjectedBA/F3cellsorBA/F3TEL-SYKcells[1]Dosage:10and100mg/kgAdministration:q.d.;for8daysResult:InhibitedtumorgrowthinREC-1subcutaneousxenograftmodelat100mg/kg.REFERENCES[1].SuWG,etal.PreparationofpyridopyrazinederivativesforuseasSykinhibitors.WO2012167733A1.[2].NaYang,etal.HMPL-523,aNovelSYKInhibitorShowedAnti-TumorActivitiesInVitroandInVivo.Blood(2016)128(22):3970.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical