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Masofaniten (EPI-7386) is an orally active androgen receptor (AR) inhibitor with antitumor activity for the study of prostate and breast cancers.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,620 | 7-10 days | |
50 mg | $2,110 | 7-10 days | |
100 mg | $3,150 | 7-10 days |
Description | Masofaniten (EPI-7386) is an orally active androgen receptor (AR) inhibitor with antitumor activity for the study of prostate and breast cancers. |
Targets&IC50 | Androgen receptor:535 nM, LNCaP cells:0.44 μM, LNCaP95 cells:3.78 μM |
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. [1] |
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. [1] |
Alias | EPI-7386, EPI7386, Androgen receptor-IN-2 |
Molecular Weight | 535.44 |
Formula | C24H24Cl2N4O4S |
Cas No. | 2416716-62-4 |
Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (74.7 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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