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  3. EPI-7170

EPI-7170 

Cat. No.: HY-150102
Handling Instructions

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).

For research use only. We do not sell to patients.

EPI-7170 Chemical Structure

EPI-7170 Chemical Structure

CAS No. : 2139288-26-7

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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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

540.88

Formula

C22H28Cl3NO6S

CAS No.
SMILES

CC(C1=CC(Cl)=C(C(Cl)=C1)OC[[email protected]](O)CCl)(C2=CC=C(C=C2)OC[[email protected]](O)CNS(C)(=O)=O)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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EPI-7170
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HY-150102
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