PF-06952229-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPF-06952229Cat.No.:HY-136244CASNo.:1801333-55-0分?式:C??H??ClFN?O?分?量:458.91作?靶點:TGF-βReceptor作?通路:TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(108.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1791mL10.8954mL21.7908mL5mM0.4358mL2.1791mL4.3582mL10mM0.2179mL1.0895mL2.1791mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.45mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.53mM);ClearsolutionBIOLOGICALACTIVITY?物活性PF-06952229?種強(qiáng)效、選擇性和?服的TGFbR1抑制劑。PF-06952229與TGFbR1特異性結(jié)合，阻?TGFbR1介導(dǎo)的信號轉(zhuǎn)導(dǎo)。PF-06952229?種很有前途的抗腫瘤試劑(antineoplasticagent)，主?于研究實體瘤，尤其轉(zhuǎn)移性乳腺癌。IC50&TargetIC50:transforminggrowthfactor-betareceptor1(TGFbR1)[1]體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellDiscov.2022Sep20;8(1):94.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FlaviaMercerPernasetti,etal.Combinationsoftgfbinhibitorsandcdkinhibitorsforthetreatmentofbreastcancer.PatentWO2020058820A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T