[CAS NO. 227947-06-0]  EPI-001

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PRODUCTS SPECIFICATIONS [227947-06-0]

Store
Catalog
SLK-S7955
Brand
Selleck
CAS
227947-06-0

DESCRIPTION [227947-06-0]

Overview

MDLMFCD02683414
Molecular Weight394.89
Molecular FormulaC21H27ClO5
SMILESC(C)(C)(C1=CC=C(OCC(CCl)O)C=C1)C2=CC=C(OCC(CO)O)C=C2

For research use only.

Storage

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

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

EPI-001 is an N-terminal domain antagonist with of ∼6 μM and a selective modulator.

Targets

PPARγ [2]Androgen Receptor [1]
(in LNCaP cells)
~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. 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.

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.


Synonyms

1,2-Propanediol, 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-
3-[4-[1-[4-(3-Chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol
EPI 001