EPI-7170

• CAT Number: I026919
• CAS Number: 2139288-26-7
• Molecular Formula: C22H28Cl3NO6S
• Molecular Weight: 540.88
• Purity: ≥95%
• Synonyms: N-[(2R)-3-[4-[2-[3,5-dichloro-4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]propan-2-yl]phenoxy]-2-hydroxypropyl]methanesulfonamide
• InChI: InChI=1S/C22H28Cl3NO6S/c1-22(2,15-8-19(24)21(20(25)9-15)32-12-16(27)10-23)14-4-6-18(7-5-14)31-13-17(28)11-26-33(3,29)30/h4-9,16-17,26-28H,10-13H2,1-3H3/t16-,17-/m1/s1
• InChIKey: DCXVYXPVNSMWPG-IAGOWNOFSA-N
• SMILES: CC(C)(C1=CC=C(C=C1)OCC(CNS(=O)(=O)C)O)C2=CC(=C(C(=C2)Cl)OCC(CCl)O)Cl

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].
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].
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].

Reference

[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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