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EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

Catalog No. T6829Cas No. 227947-06-0

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Purity:99.28%

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EPI-001

Catalog No. T6829Cas No. 227947-06-0

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
2 mg	$30	In Stock
5 mg	$43	In Stock
10 mg	$70	In Stock
25 mg	$129	In Stock
50 mg	$213	In Stock
100 mg	$318	In Stock
200 mg	$473	In Stock
1 mL x 10 mM (in DMSO)	$47	In Stock

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Product Introduction

Bioactivity

Description	EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.
Targets&IC50	Androgen receptor:6 μM
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]
Cell Research	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).(Only for Reference)
Alias	EPI001, EPI 001

Chemical Properties

Molecular Weight	394.89
Formula	C₂₁H₂₇ClO₅
Cas No.	227947-06-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 55 mg/mL (139.28 mM), Sonication is recommended.

Ethanol: 70 mg/mL (177.3 mM)

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.5324 mL	12.6618 mL	25.3235 mL	126.6175 mL
5 mM	0.5065 mL	2.5324 mL	5.0647 mL	25.3235 mL
10 mM	0.2532 mL	1.2662 mL	2.5324 mL	12.6618 mL
20 mM	0.1266 mL	0.6331 mL	1.2662 mL	6.3309 mL
50 mM	0.0506 mL	0.2532 mL	0.5065 mL	2.5324 mL
100 mM	0.0253 mL	0.1266 mL	0.2532 mL	1.2662 mL

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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