227947-06-0
227947-06-0
Chemical Structure
EPI-001
- CAS No.: 227947-06-0
- Formula:C21H27ClO5
- Molecular Weight:394.89
IUPAC Name: 3-(4-(2-(4-(3-chloro-2-hydroxypropoxy)phenyl)propan-2-yl)phenoxy)propane-1,2-diol
InChIKey: HDTYUHNZRYZEEB-UHFFFAOYSA-N
SMILES: OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1
Biological Activity: EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 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 is active against castration-resistant prostate cancer[1][2][3].
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EPI-001 | 99.34% | EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 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 is active against castration-resistant prostate cancer. | ||||||||||||||||||||
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EPI-001 (Standard) | ≥98% | EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 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 is active against castration-resistant prostate cancer. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
