227947-06-0
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
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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 |
| 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 |
|---|---|
| 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% |