Bosutinib-SKI-606-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBosutinibCat.No.:HY-10158CASNo.:380843-75-4Synonyms:SKI-606分?式:C??H??Cl?N?O?分?量:530.45作?靶點(diǎn):Src;Bcr-Abl;Autophagy作?通路:ProteinTyrosineKinase/RTK;Autophagy儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥46mg/mL(86.72mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8852mL9.4260mL18.8519mL5mM0.3770mL1.8852mL3.7704mL10mM0.1885mL0.9426mL1.8852mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.71mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.92mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.71mM);ClearsolutionBIOLOGICALACTIVITY?物活性Bosutinib?種?服Src/Abl酪氨酸激酶抑制劑，IC50分別為1.2nM和1nM。IC50&TargetIC50:1.2nM(Src),1nM(Abl)[1]體外研究Bosutinib(SKI-606)isanactiveinhibitorofBcr-Ablinseveralchronicmyelogenousleukemiacelllines,withIC50valuesinthelownanomolarrange[2].CellProliferationAssay[2]CellLine:TheleukemicBcr-Abl+celllines(KCL22,K562,KU812,andLama84)Concentration:0.1μmol/LIncubationTime:72hResult:InhibitedseveralhumanCMLderivedcelllineswithIC50valuesrangingfrom1to20nmol/L體內(nèi)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?邊的抑制劑?師www.MedChemE戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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