EPI-7170
Names
[ CAS No. ]:
2139288-26-7
[ Name ]:
EPI-7170
Biological Activity
[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].
[Related Catalog]:
[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].
[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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C22H28Cl3NO6S
[ Molecular Weight ]:
540.88