EPI-001

Names

[ Name ]:
EPI-001

[Synonym ]:
BADGE*H2O*HCl
3-(4-{2-[4-(3-Chloro-2-hydroxypropoxy)phenyl]-2-propanyl}phenoxy)-1,2-propanediol
1,2-Propanediol, 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-
EPI-001
BADGE-HCl-H2O

Biological Activity

[Description]:

EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Signaling Pathways >> Others >> Androgen Receptor

[Target]

IC50: 6 μM (AR NTD)[1]

[In Vitro]

EPI-001 (5-100 μM; 7 d) inhibits PCa/CRPC cell growth in a dose-dependent manner[2]. EPI-001 (50 μM) inhibits endogenous AR mRNA and protein expression in PCa and CRPC cell lines[2]. EPI-001 (50 μM) inhibits transcriptional activity of both AR TAU1 and TAU5[2]. Cell Proliferation Assay[2] Cell Line: PCa, CRPC, PC-3, DU 145, and T47D cell lines Concentration: 0, 5, 10, 25, 50, 100 μM Incubation Time: 7 days Result: Inhibited growth of LNCaP cells at low concentrations. Inhibited growth of AR-negative PC-3 and DU 145 cell lines as well as the T47D breast carcinoma cell line. Western Blot Analysis[2] Cell Line: LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR-R1 cells Concentration: 50 μM Incubation Time: 8-16 hours Result: Decreased expression of full-length AR protein to varying degrees.

[In Vivo]

EPI-00 (20 mg/kg; i.v. every 5 d for 25 d) inhibits the growth of tumors and has no general toxicity in vivo[1]. EPI-00 (50 mg/kg; i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth[1]. Animal Model: Male NOD-SCID mice (6-8 weeks) bearing LNCaP[1] Dosage: 20 mg/kg Administration: I.v. every 5 days for 25 days Result: Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks. Did not cause general toxicity indicated by no change in animal behavior or body weight.

[References]

[1]. Andersen RJ, et, al. Regression of castrate-recurrent prostate cancer by a small-molecule inhibitor of the amino-terminus domain of the androgen receptor. Cancer Cell. 2010 Jun 15; 17(6): 535-46.

[2]. Brand LJ, et, al. EPI-001 is a selective peroxisome proliferator-activated receptor-gamma modulator with inhibitory effects on androgen receptor expression and activity in prostate cancer. Oncotarget. 2015 Feb 28; 6(6): 3811-24.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
601.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₂₇ClO₅

[ Molecular Weight ]:
394.889

[ Flash Point ]:
317.2±31.5 °C

[ Exact Mass ]:
394.154694

[ PSA ]:
79.15000

[ LogP ]:
2.98

[ Appearance of Characters ]:
white to beige

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.571

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: soluble15mg/mL, clear

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2907230001

Customs

[ HS Code ]: 2907230001

[ Summary ]:
2907230001 4,4'-(propane-2,2-diyl)diphenol VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none Lowest tariff:5.5% General tariff:30.0%

Articles

Determination of the diglycidyl ether of bisphenol A and its derivatives in canned foods.

J. Agric. Food Chem. 47 , 1965, (1999)

Migration of the diglycidyl ether of bisphenol A (DGEBA) to food from can enamels and can pull-top seals is reported. Derivatives of DGEBA are also determined in some foods. Levels of DGEBA in the foo...

M. Biedermann et al.

Mitt. Geb. Lebensmittelunters. Hyg. 90 , 177, (1999)

Related Compounds

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