Lifirafenib-BGB-283-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELifirafenibCat.No.:HY-18957CASNo.:1446090-79-4Synonyms:BGB-283分⼦式:C₂₅H₁₇F₃N₄O₃分⼦量:478.42作⽤靶点:EGFR;Raf作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK;MAPK/ERKPathway储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(209.02mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0902mL10.4511mL20.9021mL5mM0.4180mL2.0902mL4.1804mL10mM0.2090mL1.0451mL2.0902mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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%salineSolubility:≥2.5mg/mL(5.23mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.23mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Lifirafenib(BGB-283)新型⾼效的Raf激酶和EGFR抑制剂，对重组BRafV600E和EGFR的IC50值分别为23和29nM。IC50&TargetEGFRBRafV600EEGFRL858R/T790M29nM(IC50)23nM(IC50)495nM(IC50)体外研究Lifirafenib(BGB-283)potentlyinhibitsBRafV600E-activatedERKphosphorylationandcellproliferation.ItdemonstratesselectivecytotoxicityandpreferentiallyinhibitsproliferationofcancercellsharboringBRafV600EandEGFRmutation/amplification.InBRafV600Ecolorectalcancercelllines,Lifirafenib(BGB-283)effectivelyinhibitsthereactivationofEGFRandEGFR-mediatedcellproliferation[1].体内研究Lifirafenib(BGB-283)treatmentleadstodose-dependenttumorgrowthinhibitionaccompaniedbypartialandcompletetumorregressionsinbothcellline-derivedandprimaryhumancolorectaltumorxenograftsbearingBRafV600Emutation[1].PROTOCOLCellAssay[1]Melanoma,colon,breast,andlungcancercellsarelefttoattachfor16hoursandthentreatedwitha10-pointdilutionseriesinduplicate.CellTiter-Gloreagentisaddedineachwell.Mixtureismixedonanorbitalshakerfor2minutestoallowcelllysing,followedby10minutesincubationatroomtemperaturetoallowdevelopmentandstabilizationofluminescentsignal.LuminescentsignalismeasuredusingPHERAstarFSreader.EC50valuesforcellviabilityaredetermined[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Whentheaveragetumorsizereaches110to200mm3,micearerandomizedtotreatmentgroupsandAdministration[1]treatedtwiceperdayoroncedailybyoralgavage(p.o.)withvehiclealoneor2.5to30mg/kgofBGB-283.Ascontrol,micearetreatedwitherlotinib(100mg/kgqd)orcetuximab(40mg/kgtwiceweekly).Lifirafenib(BGB-283)anderlotinibareformulatedatthedesiredconcentrationasahomogenoussuspensionin0.5%(w/v)methylcelluloseinpurifiedwater.Cetuximabisformulatedbydilutingtheinjectionsolutionwithsalinebeforedosing[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JMedVirol.2022Oct17.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TangZ,etal.BGB-283,aNovelRAFKinaseandEGFRInhibitor,DisplaysPotentAntitumorActivityinBRAF-MutatedColorectalCancers.MolCancerTher.2015Oct;14(10):2187-97.McePdfHeightCaution:Producth