Masofaniten

SKU: orb1744520

Description

Masofaniten (EPI-7386) is an oral, non-competitive androgen receptor (AR) inhibitor under investigation for prostate and breast cancer research. It demonstrates antitumor activity in both in vitro assays and in vivo xenograft models, showing potential against resistant disease forms.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2416716-62-4
• MW: 535.44
• Purity: 98.42% (May vary between batches)
• Formula: C₂₄H₂₄Cl₂N₄O₄S
• SMILES: N#CC1=CC(=CC(Cl)=C1OCCCl)C(C2=CC=C(OCC3=NC(=NC=C3)NS(=O)(=O)C)C=C2)(C)C
• Target: Androgen Receptor
• Solubility: 10% DMSO+90% Corn Oil:4 mg/mL (7.47 mM);DMSO:40 mg/mL (74.7 mM)

Bioactivity

• Target IC50:
  Androgen receptor:535 nM|LNCaP cells:0.44 μM|LNCaP95 cells:3.78 μM
• In Vivo:
  Masofaniten was able to partially inhibit tumor growth in NCG mice bearing LNCaP tumors after oral administration at a dose of 60 mg/kg. In male CD-1 mice, a single oral administration of Masofaniten at 5 mg/kg exhibited a half-life of 8.1 hours, a maximum concentration (Cmax) of 2673.3 ng/mL, and a bioavailability (F (%)) of 33.6.
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• In Vitro:
  In the androgen-induced PSA-luciferase assay, Masofaniten effectively inhibited androgen binding to the androgen receptor with an IC50 value of 535 nM. In LNCaP and LNCaP95 cells, Masofaniten showed an inhibitory effect on cell proliferation with IC50 values of 0.44 μM and 3.78 μM, respectively. In addition, Masofaniten showed good metabolic stability in liver microsomes with a half-life of more than 120 min, while the half-life in hepatocytes was more than 360 min.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AndrogenReceptor, Androgen receptor-IN-2, androgen receptor, Androgen Receptor, EPI7386, EPI-7386, Masofaniten

Compound Identifiers

PubChem CID

146484310