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Purity: ≥98%
EPI-001 (EPI001; EPI 001) is a novel, potent small-molecule antagonist of AR-androgen receptor N-terminal domain (NTD) with potential antineoplastic activity. It inhibits AR-NTD with an IC50 of ∼6 μM and also serves as a selective PPAR-gamma modulator. AR is involved in mediating the actions of male sex steroids and over-expression of AR may lead to hormone-refractory prostate cancer.
| ln Vitro |
In a dose-dependent manner, EPI-001 (5-100 μM; 7 d) suppresses the development of PCa/CRPC cells [2]. In PCa and CRPC cell lines, endogenous AR mRNA and protein expression are inhibited by EPI-001 (50 μM) [2]. AR TAU1 and TAU5 transcriptional activity is inhibited by EPI-001 (50 μM) [2].
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| ln Vivo |
In vivo tumor growth is inhibited by EPI-00 (20 mg/kg; iv every 5 days for 25 days) without causing general toxicity [1]. The androgen axis is blocked by EPI-00 (50 mg/kg; IV), which also prevents androgen-dependent tumor growth [1].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: PCa, CRPC, PC-3, DU 145, and T47D cell lines Tested Concentrations: 0, 5, 10, 25, 50, 100 μM Incubation Duration: 7 days Experimental Results: 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 Types: LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR -R1 cells Tested Concentrations: 50 μM Incubation Duration: 8-16 hrs (hours) Experimental Results: diminished expression of full-length AR protein to varying degrees. |
| Animal Protocol |
Animal/Disease Models: Male NOD-SCID (severe combined immunodeficient) mouse (6-8 weeks) bearing LNCaP[1]
Doses: 20 mg/kg Route of Administration: Iv every 5 days for 25 days Experimental Results: decreased 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. [3]. Mol ED, et, al. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor. ACS Chem Biol. 2016 Sep 16;11(9):2499-505. |
| Molecular Formula |
C21H27CLO5
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| Molecular Weight |
394.89
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| CAS # |
227947-06-0
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| Related CAS # |
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| SMILES |
ClC([H])([H])C([H])(C([H])([H])OC1C([H])=C([H])C(=C([H])C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])(C([H])([H])O[H])O[H])O[H]
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| InChi Key |
HDTYUHNZRYZEEB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27ClO5/c1-21(2,15-3-7-19(8-4-15)26-13-17(24)11-22)16-5-9-20(10-6-16)27-14-18(25)12-23/h3-10,17-18,23-25H,11-14H2,1-2H3
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| Chemical Name |
3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5324 mL | 12.6618 mL | 25.3235 mL | |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL | |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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