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  • DC Chemicals Limited
  • China
  • Product Name: EPI-001
  • Price: $450.0/100mg $800.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

227947-06-0

227947-06-0 structure
227947-06-0 structure
  • Name: EPI-001
  • Chemical Name: 3-[4-[2-[4-(3-chloro-2-hydroxypropoxy)phenyl]propan-2-yl]phenoxy]propane-1,2-diol
  • CAS Number: 227947-06-0
  • Molecular Formula: C21H27ClO5
  • Molecular Weight: 394.889
  • Catalog: analytical chemistry Standard Food and beverage standards
  • Create Date: 2017-12-11 06:21:58
  • Modify Date: 2024-01-06 19:16:18
  • 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].

Name 3-[4-[2-[4-(3-chloro-2-hydroxypropoxy)phenyl]propan-2-yl]phenoxy]propane-1,2-diol
Synonyms 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
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
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.

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 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
Symbol GHS07
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
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%