UT-155 - Androgen Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEUT-155Cat. No.: HY-112895CAS No.: 2031161-35-8分式: CHFNO分量: 405.35作靶点: Androgen Receptor作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 130 mg/mL (320.71 mM)H2O : 40% PEG300 5% Tw

2、een-80 45% salineSolubility: 2.17 mg/mL (5.35 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.17 mg/mL (5.35 mM); Suspended solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.17 mg/mL (5.35 mM); Clear solutionBI

3、OLOGICAL ACTIVITY物活性 UT-155种选择性的、有效的雄激素受体 (AR) 拮抗剂，与 AR-LBD 结合的 Ki 值为 267 nM。IC50 & Target Ki: 267 nM (AR-LBD) 1.体外研究 UT-155 binds to the AR-LBD at Ki of 267 nM. UT-155 potently inhibits the R1881-induced wildtype ARtransactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antago

4、nizes both wildtypeand mutant ARs comparably, enzalutamide is weaker by two fold with the W742L mutant AR relative to thewild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 geneexpression between 10 and 100 nM with 5-10-fold better potency than enzalutamide

5、 1.体内研究 Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1xenograft by 53%, while, as expected, enzalutamide has no effect on the growth of the 22RV1 tumors. Tumorweights and PSA and the expression of AR and AR-SV are significantly lower in UT-

6、155-treated animals 1.REFERENCES1. Ponnusamy S, et al. Novel Selective Agents for the Degradation of Androgen Receptor Variants to Treat Castration-Resistant ProstateCancer. Cancer Res. 2017 Nov 15;77(22):6282-6298.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-82