NVP-BHG712-BHG712-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENVP-BHG712Cat.No.:HY-13258ACASNo.:940310-85-0Synonyms:BHG712分?式:C??H??F?N?O分?量:503.48作?靶點(diǎn):EphrinReceptor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:31.25mg/mL(62.07mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9862mL9.9309mL19.8618mL5mM0.3972mL1.9862mL3.9724mL10mM0.1986mL0.9931mL1.9862mL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(4.13mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.13mM);ClearsolutionBIOLOGICALACTIVITY?物活性NVP-BHG712具有?服活性的EphB4激酶??磷酸化的抑制劑，其對EphA2和EphB4的IC50值分別為3.3nM和3nM。IC50&TargetIC50:3.3nM(EphA2),3nM(EphB4)[2].體外研究NVP-BHG712inhibitsVEGFdrivenvesselformation,whileithasonlylittleeffectsonVEGFreceptor(VEGFR)activity.ThedatasuggestsaclosecrosstalkbetweentheVEGFRandEphRsignalingduringvesselformation[2].體內(nèi)研究NVP-BHG712(3,10and30mg/kg,p.o.,daily)inhibitsVEGFdriventissuegrowthandangiogenesis[2].AnimalModel:Micearryingchambers[1].Dosage:3,10and30mg/kg.Administration:P.O.dailyfor4days.Result:SignificantlyinhibitedVEGFstimulatedtissueformationandvascularizationatdosesofdaily3mg/kg.Administrationof10mg/kg/kgp.o.wassufficienttoreverseVEGFenhancedtissueformationandvesselgrowth.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?PharmacolRes.2020Aug;158:104868.?CellDeathDis.2020Aug14;11(8):632.?Phytomedicine.2021,153503.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Tr?sterA,etal.NVP-BHG712:EffectsofRegioisomersontheAffinityandSelectivitytowardtheEPHrinFamily.ChemMedChem.2018Aug20;13(16):1629-1633.[2].Martiny-BaronG,etal.ThesmallmoleculespecificEphB4kinaseinhibitorNVP-BHG712inhibitsVEGFdrivenangiogenesis.Angiogenesis.2010Sep;13(3):259-67.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.For