产品
编 号:F752498
分子式:C24H24Cl2N4O4S
分子量:535.44
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1mg
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5mg
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10mg
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生物活性:
Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer.

体内研究:
Masofaniten (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors.Masofaniten (5 mg/kg, p.o., single dose, in male CD-1 mice) shows a t1/2 of 8.1 h, Cmax of 2673.3 ng/mL, F (%) of 33.6.Animal Model:LNCaP Xenografts Model
Dosage:60 mg/kg
Administration:Oral administration (p.o.)
Result:Inhibited tumor growth no obvious drug related toxicity (bodyweight change).

体外研究:
Masofaniten (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC50 of 535 nM.Masofaniten inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively).Masofaniten shows a metabolic stability in liver microsome with a t1/2 of more than 120 min, and in hepatocytes with a t1/2 of more than 360 min.
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