| Bioactivity | Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer[1]. | |||||||||
| Target | Androgen receptor | |||||||||
| Invitro | Masofaniten (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC50 of 535 nM[1].Masofaniten inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively)[1].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[1]. | |||||||||
| In Vivo | Masofaniten (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors[1].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[1]. Animal Model: | |||||||||
| Name | Masofaniten | |||||||||
| CAS | 2416716-62-4 | |||||||||
| Formula | C24H24Cl2N4O4S | |||||||||
| Molar Mass | 535.44 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Han-Jie Zhou, et al. Androgen receptor modulators and methods for their use. Patent. US20200123117A1. |
Masofaniten
CAS: 2416716-62-4 F: C24H24Cl2N4O4S W: 535.44
Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumo
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