Uzansertib-phosphate-INCB053914-phosphate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUzansertibphosphateCat.No.:HY-101870BCASNo.:2088852-47-3Synonyms:INCB053914phosphate分⼦式:C₂₆H₂₉F₃N₅O₇P分⼦量:611.51作⽤靶点:Pim作⽤通路:JAK/STATSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:5mg/mL(8.18mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6353mL8.1765mL16.3530mL5mM0.3271mL1.6353mL3.2706mL10mM---------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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥1.8mg/mL(2.94mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.8mg/mL(2.94mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.8mg/mL(2.94mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Uzansertib(INCB053914)phosphate⼀种具有⼝服活性的，ATP竞争性泛-PIM激酶抑制剂，对于PIM1，PIM2和PIM3的IC50分别为0.24nM，30nM和0.12nM。Uzansertibphosphate对多种⾎液肿瘤细胞系具有⼴泛的抗增殖活性。IC50&TargetPIM1PIM2PIM30.24nM(IC50)30nM(IC50)0.12nM(IC50)体外研究Uzansertibphosphateinhibitsproliferationinallmultiplemyeloma(MM)celllinestested,withmeanGI50valuesrangingfrom13.2nMto230.0nMinAML,MM,DLBCL,MCL,andT-ALLcelllines[1].Uzansertibphosphate(0.1,0.3,1,3,10,30,100,300,1000nM)inhibitsthephosphorylationofdownstreamPIMkinasesubstrates(p70S6K/S6and4E-BP1)inadose-dependentmannerinMOLM-16(AML),Pfeiffer(DLBCL),andKMS-12-PE/BM(MM)celllines[1].PIMkinase-mediatedphosphorylationofBADinMOLM-16andKMS-12-BMcellsisparticularlysensitivetoinhibitionbyUzansertibphosphate(meanIC50,4nMand27nM,respectively)[1].体内研究Uzansertibphosphate(25-100mg/kg;PO;twiceaday;for15days)inhibitstumorgrowthinadose-dependentmannerinmicebearingMOLM-16(AML)orKMS-12-BM(MM)[1].Uzansertibphosphatedemonstratesadose-dependentinhibitionofBADphosphorylationrelativetovehicleat4hourspostdose(MOLM-16tumors,IC50=70nM;KMS-12-BMtumors,IC50=145nM)[1].AnimalModel:Femaleimmunecompromised(severecombinedimmunodeficiency[SCID])mice(5-9weeksofage)bearingMOLM-16(AML)orKMS-12-BM(MM)[1]Dosage:25,50,75,100mg/kgAdministration:PO;twiceaday;for15daysResult:Inhibitedtumorgrowthinadose-dependentmannerinmice.REFERENCES[1].KoblishH,etal.PreclinicalcharacterizationofINCB053914,anovelpan-PIMkinaseinhibitor,aloneandincombinationwithanticanceragents,inmodelsofhematologicmalignancies.PLoSOne.2018Jun21;13(6):e0199108.McePdfHeightCaution:Producthasnotbeenfullyvalidated