EPI-001

製品コードS7955 バッチS795501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₁H₂₇ClO₅

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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, this compound inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. ^[1] In LNCaP cells, it 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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LNCaP cells
	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, this compound 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.

参考

https://pubmed.ncbi.nlm.nih.gov/20541699/
https://pubmed.ncbi.nlm.nih.gov/25669987/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Prebiotic stachyose inhibits PRDX5 activity and castration-resistant prostate cancer development [ Int J Biol Macromol, 2024, 278(Pt 3):134844]	PubMed: 39168191
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。