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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C15H12F4N4O2 |
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分子量 | 356.27 | CAS No. | 2168525-92-4 | |
Solubility (25°C)* | 体外 | DMSO | 71 mg/mL (199.28 mM) | |
Ethanol | 71 mg/mL (199.28 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer. |
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in vitro | UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vitro proliferation. UT-34 promotes a conformation that is distinct from the LBD-binding competitive antagonist enzalutamide and degrades the AR through the ubiquitin proteasome mechanism. UT-34 has a broad safety margin and exhibits no cross-reactivity with Gprotein-coupled receptor kinase and nuclear receptor family members.[1] |
in vivo | UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vivo growth of enzalutamide-sensitive and -resistant prostate cancer xenografts. In preclinical models, UT-34 induces the regression of enzalutamide-resistant tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors.[1] |
細胞アッセイ | 細胞株 | LNCaP, PC-3, HEK-293, ZR-75-1, MDA-MB-453, VCaP, 22RV1, and COS7 cell lines |
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濃度 | 0.1 μM, 1 μM, 10 μM | |
反応時間 | 30 min, 24 h, 48 h | |
実験の流れ | LNCaP cells are maintained in 1% charcoal-stripped serum-containing mediumfor two days. Cells are treated with the indicated doses of UT-34 in the presence of 0.1 nmol/L R1881 for 24 hours, protein is extracted, and Western blot analysis for AR and actin is performed. |
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動物実験 | 動物モデル | NSG mice with MR49F xenograft |
投薬量 | 20 mg/kg, 40 mg/kg | |
投与方法 | Oral gavage |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。