PND-1186-VS-4718-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPND-1186Cat.No.:HY-13917CASNo.:1061353-68-1Synonyms:VS-4718;SR-2516分⼦式:C₂₅H₂₆F₃N₅O₃分⼦量:501.5作⽤靶点:FAK;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥34mg/mL(67.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9940mL9.9701mL19.9402mL5mM0.3988mL1.9940mL3.9880mL10mM0.1994mL0.9970mL1.9940mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.99mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.99mM);Clearsolution3.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.99mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PND-1186(VS-4718)⼀种有效的，⾼特异性的，可逆的FAK抑制剂，IC50为1.5nM。PND-1186选择性促进肿瘤细胞凋亡(apoptosis)[1]。IC50&TargetIC50:1.5nM(FAK)[1]体外研究PND-1186hasanIC50of~100nMinbreastcarcinomacellsasdeterminedbyanti-phospho-specificimmunoblottingtoFAKTyr-397[1].Inmurine4T1breastcarcinomacells,FAKisimportantinpromotinganinvasiveandmetastaticcellphenotype.IncreasingconcentrationsofPND-1186(0.1to1.0µM)addedto4T1cellsinhibitsFAKTyr-397phosphorylation(pY397)andresultsinelevatedlevelsoftotalFAKproteinwithin1h[1].WesternBlotAnalysis[1]CellLine:4T1breastcarcinomacellsConcentration:0.1,0.2,0.4,0.6and1.0µMIncubationTime:1hourResult:InhibitedFAKTyr-397phosphorylation(pY397)andresultedinelevatedlevelsoftotalFAKprotein.体内研究PND-1186(30mg/kgor100mg/kg;subcutaneously;injectedsubcutaneouslyintheneckregion)inhibits4T1subcutaneoustumorgrowthbyinductionofapoptosis[1].AnimalModel:BALB/cmice[1]Dosage:30mg/kgor100mg/kgAdministration:Injected(100µL)subcutaneouslyintheneckregion;every12h(twice-daily,b.i.d.)for5days.Result:100mg/kgtreatmentsignificantlyreducedfinal4T1tumorweight2-foldwhereas30mg/kgtreatmentslightlyreducedfinaltumorweightbutwasnotsignificantlydifferentcomparedtocontrol.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•CancerCell.2019Mar18;35(3):457-472.e5.•ClinCancerRes.2019Jul15;25(14):4552-4566.•JExpClinCancerRes.2022Jun3;41(1):193.•bioRxiv.2020Apr.•HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].TanjoniI,etal.PND-1186FAKinhibitorselectivelypromotestumorcellapoptosisinthree-dimensionalenvironments.CancerBiolTher.2010May15;9(10):764-77.McePdfHeightCaution:Producthasnotbeenfullyvalidate