Catalog No.: PC-49412Not For Human Use, Lab Use Only.
EPI-7170 is a potent next-generation analog of Ralaniten (EPI-002) and inhibitor of androgen receptor N-terminal domain (AR-NTD), inhibits androgen-induced PSA-luciferase activity in transiently transfected LNCaP cells with IC50 of 1.08 uM.
EPI-7170 is a potent next-generation analog of Ralaniten (EPI-002) and inhibitor of androgen receptor N-terminal domain (AR-NTD), inhibits androgen-induced PSA-luciferase activity in transiently transfected LNCaP cells with IC50 of 1.08 uM.
EPI-7170 has approximately 10 times better potency for inhibiting AR transcriptional activity compared to ralaniten.
EPI-7170 selectively inhibits the DNA damage repair (DDR) pathway in prostate cancer cells that express both full-length AR and AR-Vs, whereas enzalutamide has no effect.
EPI-7170 increase levels of γH2AX whereas enzalutamide has little added benefit in LNCaP95 cells.
EPI-7170 specifically inhibits AR-dependent proliferation and tumor growth.
EPI-7170 (25 mg/kg, oral) has antitumor activity on CRPC xenografts driven by AR and AR-Vs in vivo.
