| Description |
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC)[1].
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| Related Catalog |
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| In Vitro |
EPI-7170 (0-12 μM, 24 or 48 h) inhibits cell proliferation in VCaP-ENZR and C4-2B-ENZR cells, also enhances the effect of enzalutamide which has a lower IC 50 when bound to EPI-7170[1]. EPI-7170 (0-20 μM, 24 or 48 h) synergistically inhibits androgen receptor (AR) transcriptional activity in ENZR cells expressing androgen receptor splice variant-7 (AR-V7) with enzalutamide[1]. EPI-7170 (3.5 μM, 48 h) results in an increase in G1 phase and a decrease in S phase, and reduces the expression levels of CDK4, cyclin D1 and cyclin A2 proteins[1].
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| In Vivo |
EPI-7170 (oral administration, 30 mg/kg, daily, 31 days) has some anti-tumor activity and can be combined with enzalutamide in male NOD/SCID mice[1]. Animal Model: 6-8 week old male NOD/SCID mice infected with VCaP-ENZR cells[1] Dosage: 30 mg/kg Administration: Oral administration; daily; 31 days Result: Significantly reduced tumor volume and decreased levels of FL-AR and AR-V7 in harvested xenografts.
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| References |
[1]. Hirayama Y, et al. Combination therapy with androgen receptor N-terminal domain antagonist EPI-7170 and enzalutamide yields synergistic activity in AR-V7-positive prostate cancer. Mol Oncol. 2020 Oct;14(10):2455-2470.
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