GSK2606414-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2606414Cat.No.:HY-18072CASNo.:1337531-36-8分⼦式:C₂₄H₂₀F₃N₅O分⼦量:451.44作⽤靶点:PERK;Autophagy;Apoptosis作⽤通路:CellCycle/DNADamage;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(221.51mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2151mL11.0757mL22.1513mL5mM0.4430mL2.2151mL4.4303mL10mM0.2215mL1.1076mL2.2151mL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：0.5%HPMC>>0.2%Tween801/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:3.33mg/mL(7.38mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.54mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.54mM);Suspendedsolution;Needultrasonic4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(5.54mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK2606414可渗透细胞且有⼝服活性的蛋⽩激酶R样内质⽹(ER)激酶(PERK)抑制剂，IC50值为0.4nM。IC50&TargetEIF2AK3(PERK)EIF2AK1(HRI)EIF2AK2(PKR)0.4nM(IC50)420nM(IC50)696nM(IC50)体外研究GSK2606414inhibitsPERKactivationincells[1].体内研究GSK2606414(50and150mg/kg,p.o.)inhibitsthegrowthofahumantumorxenograftinmice[1].PROTOCOLAnimalExponentiallygrowingBxPC3tumorcells(10×106cells/mouse)fromcellcultureareimplantedAdministration[1]subcutaneouslyintotherightflankoffemalenudemice.Sixteendaysafterimplantation,micewith-200mm3tumorsarerandomizedintovarioustreatmentgroups(n=8mice/group).Animalsareorallytreatedwithvehicle(0.5%hydoxypropylmethylcellulose,0.1%Tween80inwater,pH4.8),compoundat50or150mg/kg,b.i.d.for21days.Tumorvolumeismeasuredtwiceweeklywithcalipersandcalculated.Resultsarerepresentedaspercentinhibitiononcompletionofdosing,whichis100[1-(averagegrowthofdrug-treatedpopulation)/(averagegrowthofvehicle-treatedcontrolpopulation)].Statisticalanalysisisperformedusingatwo-tailedttest.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellMetab.2021Mar2;33(3):598-614.e7.•CellHostMicrobe.2017Dec13;22(6):766-776.e4.•NatImmunol.2022Jul;23(7):1021-1030.•Biomaterials.2021,120757.•SciAdv.2021Jun16;7(25):eabf8577.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].AxtenJM,etal.Discoveryof7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(GSK2606414),apotentandselectivefirst-in-classinhibitorofproteinkinaseR(PKR)-likeendoplasmicreticulu[2].ZhangM,etal.InhibitingthePlasmodiumeIF2αKinasePK4PreventsArtemisinin-InducedLatency.CellHostMicrobe.2017Dec13;22(6):766-776.e4.McePdfHeightCaution:Producthasnotbeenf