CAS NO: | 227947-06-0 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 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) | |
Other info | Chemical Name: 3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol InChi Key: HDTYUHNZRYZEEB-UHFFFAOYSA-N 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 SMILES Code: OCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1 |
Synonyms | EPI-001; EPI 001; EPI001 |
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. 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. |