Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETD-165Cat.No.:HY-130714CASNo.:2305936-56-3分?式:C??H??N?O?S分?量:870.07作?靶點(diǎn):PROTACs作?通路:PROTAC儲(chǔ)存?式:-20°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:50mg/mL(57.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.1493mL5.7467mL11.4933mL5mM0.2299mL1.1493mL2.2987mL10mM0.1149mL0.5747mL1.1493mL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?。BIOLOGICALACTIVITY?物活性TD-165于PROTAC技術(shù)的CRBN降解劑。TD-165包括?個(gè)CRBN配體結(jié)合團(tuán)，?個(gè)linker和?個(gè)VHL結(jié)合團(tuán)。IC50&TargetCereblon20.4nM(DC50)體外研究TD-165(0-100nM;24hours)shows50%degradationconcentration(DC50)andmaximumdegradation1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE(Dmax)valueof20.4?nMand99.6%,respectively[1].TD-165(0.1-10?μM;24hours)leadstoaconcentration-dependentdecreaseinthelevelofCRBNproteinsinHEK293Tcells[1].CellViabilityAssay[1]CellLine:HEK293TcellsConcentration:0-100nMIncubationTime:24hoursResult:ExhibitedanDC50valueof20.4?nM.WesternBlotAnalysis[1]CellLine:HEK293TcellsConcentration:0.1,1,and10?μMIncubationTime:24hoursResult:DecreasedthelevelofCRBNprotein.REFERENCES[1].KimK,etal.Disorderedregionofcereblonisrequiredforefficientdegradationbyproteolysis-targetingchimera.SciRep.2019Dec23;9(1):19654.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-58955