Giredestrant-GDC-9545-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGiredestrantCat.No.:HY-109176CASNo.:1953133-47-5Synonyms:GDC-9545分?式:C??H??F?N?O分?量:522.55作?靶點:EstrogenReceptor/ERR作?通路:Others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(95.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9137mL9.5685mL19.1369mL5mM0.3827mL1.9137mL3.8274mL10mM0.1914mL0.9568mL1.9137mL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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.78mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.78mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.78mM);ClearsolutionBIOLOGICALACTIVITY?物活性Giredestrant(GDC-9545)?種?甾體雌激素受體(ER)配體，?服有效的，選擇性ER拮抗劑。Giredestrant可以在ER配體結(jié)合域內(nèi)與雌?醇(Estradiol)競爭結(jié)合并誘導構(gòu)象變化。Giredestrant具有抗腫瘤活性。IC50&TargetER體外研究Giredestrant(GDC-9545)isanovelERantagonistthatcombinesdesirablemechanisticandpre-clinicalDMPKattributes.ThehighlypotentinvivoefficacyofGiredestrantlikelyarisesduetotheparticularcombinationofhighbindingpotency,fullsuppressionofERsignaling,andanimprovedDMPKprofile[1].REFERENCES[1].CMetcalfe,etal.AbstractP5-04-07:GDC-9545:AnovelERantagonistandclinicalcandidatethatcombinesdesirablemechanisticandpre-clinicalDMPKattributesMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-