product name EPI-001
Description: EPI-001 is a small-molecule androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator. EPI-001 targets the amino terminal domain of the AR and inhibit the protein-protein interactions which are necessary for AR transcriptional activity. The androgen receptor (AR) is involved in mediating the actions of male sex steroids. Amplification and over-expression of androgen receptor gene may result in hormone-refractory prostate cancer.
References: Cancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24.
394.89
Formula
C21H27ClO5
CAS No.
227947-06-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (200.1 mM)
Water: <1 mg/mL
Ethanol: 79 mg/mL (200.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394702
| In Vitro |
In vitro activity: EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. Kinase Assay: Cell Assay: LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions). |
|---|---|
| In Vivo | In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. |
| Animal model | Male mice bearing LNCaP s.c. xenografts |
| Formulation & Dosage | Dissolved in DMSO; 50 mg/kg; i.v. injection |
| References | Cancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24. |
Related Posts
product name EPI-001
Description: EPI-001 is a small-molecule androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator. EPI-001 targets the amino terminal domain of the AR and inhibit the protein-protein interactions which are necessary for AR transcriptional activity. The androgen receptor (AR) is involved in mediating the actions of male sex steroids. Amplification and over-expression of androgen receptor gene may result in hormone-refractory prostate cancer.
References: Cancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24.
394.89
Formula
C21H27ClO5
CAS No.
227947-06-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 79 mg/mL (200.1 mM)
Water: <1 mg/mL
Ethanol: 79 mg/mL (200.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19394702
| In Vitro |
In vitro activity: EPI-001 blocks transactivation of the AR NTD, interacts with the AF-1 region, inhibits protein-protein interactions with AR, and reduces AR interaction with androgen-response elements on target genes. In LNCaP cells, EPI-001 inhibits both androgen-dependent and androgen-independent (OCM-induced) cell proliferation. In LNCaP cells, EPI-001 also acts as a PPAR-gamma modulator to result in inhibition of androgen receptor expression and activity, which inhibits prostate cancer growth. Kinase Assay: Cell Assay: LNCaP cells are treated with bicalutamide (BIC) or EPI-001 for 1 hr before the addition of R1881 (0.1 nM) for 4 days. LNCaP cells are treated with OCM (50%) with, or without, EPI-001 for 3 days (serum-free, androgen-free, phenol red-free conditions). |
|---|---|
| In Vivo | In male mice bearing CRPC LNCaP s.c. xenografts, EPI-001 (50 mg/kg, i.v.) blocks the androgen-axis and inhibits androgen-dependent tumor growth by reducing proliferation and increasing apoptosis. |
| Animal model | Male mice bearing LNCaP s.c. xenografts |
| Formulation & Dosage | Dissolved in DMSO; 50 mg/kg; i.v. injection |
| References | Cancer Cell. 2010 Jun 15;17(6):535-46; Oncotarget. 2015 Feb 28;6(6):3811-24. |