Bosutinib-SKI-606-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBosutinibCat.No.:HY-10158CASNo.:380843-75-4Synonyms:SKI-606分⼦式:C₂₆H₂₉Cl₂N₅O₃分⼦量:530.45作⽤靶点:Src;Bcr-Abl;Autophagy作⽤通路:ProteinTyrosineKinase/RTK;Autophagy储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:≥46mg/mL(86.72mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8852mL9.4260mL18.8519mL5mM0.3770mL1.8852mL3.7704mL10mM0.1885mL0.9426mL1.8852mL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(protectfromlight)。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.71mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.92mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Bosutinib⼀种⼝服Src/Abl酪氨酸激酶抑制剂，IC50分别为1.2nM和1nM。IC50&TargetIC50:1.2nM(Src),1nM(Abl)[1]体外研究Bosutinib(SKI-606)isanactiveinhibitorofBcr-Ablinseveralchronicmyelogenousleukemiacelllines,withIC50valuesinthelownanomolarrange[2].CellProliferationAssay[2]CellLine:TheleukemicBcr-Abl+celllines(KCL22,K562,KU812,andLama84)Concentration:0.1μmol/LIncubationTime:72hResult:InhibitedseveralhumanCMLderivedcelllineswithIC50valuesrangingfrom1to20nmol/L体内研究Bosutinib(oralgavage;75mg/kgtwicedailyor150mg/kgoncedaily)hasactivityagainsthumanKU812xenograftsinnudemice.Bosutinib(150mg/kg;oncedaily,5daysweekly)hasactivityagainstsyngeneicBcr-AblWTandmutantBa/F3xenografts[2].AnimalModel:KU812CMLxenograftmodel[2]Dosage:75mg/kgtwicedailyor150mg/kgoncedailyAdministration:Bosutinib(oralgavage;75mg/kgtwicedailyor150mg/kgoncedaily)Result:Hadthetherapeuticactivityandproducedadose-andschedule-dependentweightloss.AnimalModel:SyngeneicBcr-AblWTandmutantBa/F3xenografts[2]Dosage:150mg/kgAdministration:Bosutinib(150mg/kg;oncedaily,5daysweekly)Result:Decreasedtherateoftumorgrowthandprolongedevent-freesurvivalofmice.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•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•Biomolecules.2022Jun11;12(6):819.•FrontPharmacol.2021Mar8;12:644342.•TargetOncol.2020Oct;15(5):659-671.•SaudiJBiolSci.6December2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JorgeECortes,etal.Bosutinibversusimatinibinnewlydiagnosedchronic-phasechronicmyeloidleukemia:resultsfromtheBELAtrial.JClinOncol.2012Oct1;30(28):3486-92.[2].MiriamPuttini,etal.InvitroandinvivoactivityofSKI-606,anovelSrc-Ablinhibitor,againstimatinib-resistantBcr-Abl+neoplasticcells.CancerRes.2006Dec1;66(23):11314-22.McePdfHeightCaution:Producthasnotbeenfull