Flumatinib-HHGV678-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFlumatinibCat.No.:HY-13904CASNo.:895519-90-1Synonyms:HHGV678分⼦式:C₂₉H₂₉F₃N₈O分⼦量:562.59作⽤靶点:Bcr-Abl;c-Kit;PDGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(177.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7775mL8.8875mL17.7749mL5mM0.3555mL1.7775mL3.5550mL10mM0.1777mL0.8887mL1.7775mL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：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(3.70mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Flumatinib(HHGV678)⼀种具有⼝服活性的选择性Bcr-Abl抑制剂，对c-Abl，PDGFRβ和c-Kit的IC50分别为1.2nM，307.6nM和665.5nM[1]。IC50&TargetIC50Value:1.2nM(c-Abl);307.6nM(PDGFRβ);2662nM(c-Kit)[1].体外研究Flumatinib(HH-GV-678)canpredominantlyinhibittheautophosphorylationofBcr-AblinK562cell.Inhigherconcentration,Flumatinibcaninhibitthephosphorylationofc-KitinMo7ecellandthephosphorylationofPDGFRinSwiss3T3cell,however,FlumatinibhasnoorlittleeffectonothertyrosinekinaseincludingEGFR,KDR,c-SrcandHER2[1].Flumatinib(HHGV678)effectivelyovercamethedrugresistanceofcertainKITmutantswithactivationloopmutations(i.e.,D820G,N822K,Y823D,andA829P)[2].REFERENCES[1].LuoH,etal.HH-GV-678,anovelselectiveinhibitorofBcr-Abl,outperformsimatinibandeffectivelyoverridesimatinibresistance.Leukemia.2010Oct;24(10):1807-9.[2].ZhaoJ,etal.Flumatinib,aselectiveinhibitorofBCR-ABL/PDGFR/KIT,effectivelyovercomesdrugresistanceofcertainKITmutants.CancerSci.2013Nov10.[3].GongA,etal.Metabolismofflumatinib,anovelantineoplastictyrosinekinaseinhibitor,inchronicmyelogenousleukemiapatients.DrugMetabDispos.2010Aug;38(8):1328-40.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear