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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H27ClO5 |
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分子量 | 394.89 | CAS No. | 227947-06-0 | |
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (200.05 mM) | |
Ethanol | 79 mg/mL (200.05 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 | EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator. |
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in vitro | EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. [1] In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. [2] |
in vivo | In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. [1] |
細胞アッセイ | 細胞株 | LNCaP cells |
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濃度 | 10 μg/mL | |
反応時間 | 4 days | |
実験の流れ | LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions). | |
動物実験 | 動物モデル | Male mice bearing LNCaP s.c. xenografts |
投薬量 | 50 mg/kg | |
投与方法 | i.v. |
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Rational optimization of a transcription factor activation domain inhibitor [ Nat Struct Mol Biol, 2023, 30(12):1958-1969] | PubMed: 38049566 |
Effects of Oncolytic Vaccinia Viruses Harboring Different Marine Lectins on Hepatocellular Carcinoma Cells [ Int J Mol Sci, 2023, 24(4)3823] | PubMed: 36835232 |
N-glycosylation of GDF15 abolishes its inhibitory effect on EGFR in AR inhibitor-resistant prostate cancer cells [ Cell Death Dis, 2022, 13(7):626] | PubMed: 35853851 |
Oncolytic Vaccinia Virus Harboring Aphrocallistes vastus Lectin Inhibits the Growth of Hepatocellular Carcinoma Cells [ Mar Drugs, 2022, 20(6)378] | PubMed: 35736181 |
Hybrid Androgen Receptor Inhibitors Outperform Enzalutamide and EPI-001 in in vitro Models of Prostate Cancer Drug Resistance [ ChemMedChem, 2022, e202200548.] | PubMed: 36300876 |
Combined N-terminal androgen receptor and autophagy inhibition increases the antitumor effect in enzalutamide sensitive and enzalutamide resistant prostate cancer cells [ Prostate, 2019, 79(2):206-214] | PubMed: 30345525 |
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。