Acrizanib-LHA510-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAcrizanibCat.No.:HY-109020CASNo.:1229453-99-9Synonyms:LHA510分⼦式:C₂₀H₁₈F₃N₇O₂分⼦量:445.4作⽤靶点:VEGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:41.67mg/mL(93.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2452mL11.2259mL22.4517mL5mM0.4490mL2.2452mL4.4903mL10mM0.2245mL1.1226mL2.2452mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.67mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.67mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Acrizanib(LHA510)⼀种VEGFR-2的抑制剂，其对BaF3-VEGFR-2的IC50值为17.4nM。IC50&TargetVEGFR-217.4nM(IC50)体外研究AcrizanibisaVEGFR-2inhibitor,withanIC50of17.4nMforBaF3-KDR.Acrizanib(compound35)exhibits≤10%remainingkinaseactivityagainstonly13wildtypekinases:CSF1R,Kit,PDGFRα,PDGFRβ,VEGFR1,VEGFR2,VEGFR3,Fms(solubleVEGFR1),DDR1,DDR2,TIE1,andABL1(nonphosphorylated)[1].体内研究RatocularPKstudieswithAcrizanibshowsadistinctlydifferentprofilefromthatobservedwithcompound25.WhileprolongedexposureisonceagainevidentinthePEC,theAUCratiotothelevelofAcrizanibinplasmaismarkedlyincreased(>21000-foldhigherexposureinthePECthanplasmaonday11).Furthermore,unlike25,AcrizanibalsoaffordmuchimprovedretinatoplasmaAUCexposureratioafter10daysofdosing(598×forAcrizanibvs0.8×for25)[1].REFERENCES[1].AdamsCM,etal.TheDiscoveryofN-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide(Acrizanib),aVEGFR-2InhibitorSpecificallyDesignedforTopicalOcularDelivery,asaTherapyforMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear