PF-4618433-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesPF-4618433Cat.No.:HY-18312CASNo.:1166393-85-6分⼦式:C₂₄H₂₇N₇O₂分⼦量:445.52作⽤靶点:Pyk2作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:125mg/mL(280.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2446mL11.2228mL22.4457mL5mM0.4489mL2.2446mL4.4891mL10mM0.2245mL1.1223mL2.2446mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(4.67mM);Clearsolution此⽅案可获得≥2.08mg/mL(4.67mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.67mM);Clearsolution1/3此⽅案可获得≥2.08mg/mL(4.67mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.08mg/mL(4.67mM);Clearsolution此⽅案可获得≥2.08mg/mL(4.67mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性PF-4618433⼀种有效的、选择性的PYK2抑制剂，IC50值为637nM。PF-4618433可能适⽤于研究⾻质疏松症，颅和阑尾⾻骼缺损以及靶向⾻再⽣[1][2]。IC50&TargetIC50:637nM(PYK2)[1]体外研究PF-4618433(0.1-1.0μM;7days)promotesosteogenesisofhMSCcultures.PF-4618433increasesinbothalkalinephosphatase(ALP)activityandmineralizationinadependentmanner[1].PF-4618433(0.1-0.3μM;24hours)enhancesosteoblastproliferation[2].PF-4618433(0.0125-0.3μM;14or21days)enhancescalciumdepositionattheconcentrationsof0.1and0.3μM[2].CellProliferationAssay[2]CellLine:Murinebonemarrow-derivedmesenchymalstemcells(BMSC)Concentration:0.1,0.3μMIncubationTime:24hoursResult:Increasedcellproliferationactivitysignificantlywhencomparedtotheuntreatedorcontrolgroup.REFERENCES[1].SeungilH,et,al.StructuralCharacterizationofProline-RichTyrosineKinase2(PYK2)RevealsaUnique(DFG-out)ConformationandEnablesInhibitorDesign.JBiolChem.2009May8;284(19):13193-201.[2].SumanaP,et,al.APyk2InhibitorIncorporatedIntoaPEGDA-gelatinHydrogelPromotesOsteoblastActivityandMineralDeposition.BiomedMater.2019Feb27;14(2):025015.McePdfHeight2/3MedChemExpress(MCE)