R-Bicalutamide-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibraries(R)-BicalutamideCat.No.:HY-108250CASNo.:113299-40-4分?式:C??H??F?N?O?S分?量:430.37作?靶點(diǎn):AndrogenReceptor作?通路:Others儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(232.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3236mL11.6179mL23.2358mL5mM0.4647mL2.3236mL4.6472mL10mM0.2324mL1.1618mL2.3236mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(5.81mM);Clearsolution此?案可獲得≥2.5mg/mL(5.81mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請(qǐng)依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.81mM);Clearsolution1/3此?案可獲得≥2.5mg/mL(5.81mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.5mg/mL(5.81mM);Clearsolution此?案可獲得≥2.5mg/mL(5.81mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性(R)-BicalutamideBicalutamide(HY-14249)的R型對(duì)映體。(R)-Bicalutamide?種雄激素受體(AR)拮抗劑，具有抗腫瘤活性。(R)-Bicalutamide?泛?于前列腺癌的研究[1][2]。IC50&TargetAR[1]體外研究Bicalutamide(HY-14249)isavailableasaracemicmixture.TheRisomer(R-bicalutamide)hasan≈30-foldhigherbindingaffinitytotheARthantheSisomer[1].(R)-bicalutamide(0.02-20μM)reducesna?veLNCaPcellssurvivalinadose-dependent[2].CellProliferationAssay[2]CellLine:LNCaPcells,LNCaP-RbiccellsConcentration:0.02μM,0.2μM,2μM,20μMIncubationTime:144hoursResult:Reducedna?veLNCaPcellssurvivalinadose-dependent,withanIC50valueofabout7μM;exertedapoorantiproliferativeeffectonLNCaP-Rbic.體內(nèi)研究(R)-Bicalutamide(10mg/kg;i.g.;daily;for4days)hasantitumorefficacyinVCaPxenograftsmice[3].AnimalModel:CD1malenude(nu/nu)mice,withVCaPxenografts[3]Dosage:10mg/kgAdministration:Orallygavage,daily,for4consecutiveweeksResult:Suppressedtumorgrowth.REFERENCES[1].HongliLiu,etal.MolecularmechanismofR-bicalutamideswitchingfromandrogenreceptorantagonisttoagonistinducedbyaminoacidmutationsusingmoleculardynamicssimulationsandfreeenergycalculation.JComputAidedMolDes.2016Dec;30(12):1189-1200.2/3[2].SaraPignatta,etal.Prolongedexposureto(R)-bicalutamidegeneratesaLNCaPsubclonewithalterationofmitochondrialgenome.MolCellEndocrinol.2014Jan25;382(1):314-324.[3].AnnaTesei,etal.EffectofSmallMoleculesModulatingAndrogenReceptor(SARMs)inHumanProstateCancerModels.PLoSOne.2013;8(5):e62657.McePdfHeight