Masofaniten

Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer In Vitro Masofaniten (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC 50 of 535 nM. Masofaniten inhibits cell proliferation in LNCaP and LNCaP95 cells (IC 50 : 0.44 μM, 3.78 μM respectively). Masofaniten shows a metabolic stability in liver microsome with a t 1/2 of more than 120 min, and in hepatocytes with a t 1/2 of more than 360 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 t 1/2 of 8.1 h, C max of 2673.3 ng/mL, F (%) of 33.6 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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). Form:Solid IC50& Target:Androgen receptor

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