For research use only. Not for therapeutic Use.
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC)[1][2].
EPI-002 (5-35 μM; 2-3 days) reduces AR-dependent proliferation of LNCaP cells, and has no effect on the viability of PC3 human prostate cancer cells that do not express functional AR[1].
Ralaniten (10-35 μM; 4 h) inhibits transactivation of the AR N-terminal domain (NTD) induced by forskolin in LNCaP cells[1].
EPI-002 (100 mg/kg; p.o. twice daily for 28 days) inhibits the VCaP tumor growth in castrated mice[1].
| Catalog Number | I035427 |
| CAS Number | 1203490-23-6 |
| Synonyms | (2R)-3-[4-[2-[4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]propan-2-yl]phenoxy]propane-1,2-diol |
| Molecular Formula | C21H27ClO5 |
| Purity | ≥95% |
| InChI | 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/t17-,18-/m1/s1 |
| InChIKey | HDTYUHNZRYZEEB-QZTJIDSGSA-N |
| SMILES | CC(C)(C1=CC=C(C=C1)OCC(CO)O)C2=CC=C(C=C2)OCC(CCl)O |
| Reference | [1]. Myung JK, et, al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013 Jul;123(7):2948-60. [2]. Yang YC, et, al. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2016 Sep 1;22(17):4466-77. |
