PF-06952229-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-06952229Cat.No.:HY-136244CASNo.:1801333-55-0分⼦式:C₂₃H₂₄ClFN₄O₃分⼦量:458.91作⽤靶点:TGF-βReceptor作⽤通路:TGF-beta/Smad储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(108.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1791mL10.8954mL21.7908mL5mM0.4358mL2.1791mL4.3582mL10mM0.2179mL1.0895mL2.1791mL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%salineSolubility:≥2.5mg/mL(5.45mM);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%cornoilSolubility:≥2.08mg/mL(4.53mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-06952229⼀种强效、选择性和⼝服的TGFbR1抑制剂。PF-06952229与TGFbR1特异性结合，阻⽌TGFbR1介导的信号转导。PF-06952229⼀种很有前途的抗肿瘤试剂(antineoplasticagent)，主⽤于研究实体瘤，尤其转移性乳腺癌。IC50&TargetIC50:transforminggrowthfactor-betareceptor1(TGFbR1)[1]体内研究PF-06952229(oralgavage;30mg/kg;twicedaily;21days)combineswithPalbociclib21daysresultsinanimprovedinhibitionofpSMAD2intheMCF7ER+xenograftbreastcancertumormodel.ThiscombinationalsoleadstoasignificantincreaseinsurvivalrelativetoPF-06952229monotherapy[1].AnimalModel:MCF-7ER+HER2-xenograftbreastcancertumormodel[1]Dosage:30mg/kgAdministration:Oralgavage;twicedaily;44daysResult:ResultedinanincreaseintumorgrowthinhibitionwhencombinedwithPalbociclib.户使⽤本产品发表的科研⽂献•CellDiscov.2022Sep20;8(1):94.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FlaviaMercerPernasetti,etal.Combinationsoftgfbinhibitorsandcdkinhibitorsforthetreatmentofbreastcancer.PatentWO2020058820A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T