Masofaniten

• CAT Number: I042657
• CAS Number: 2416716-62-4
• Molecular Formula: C24H24Cl2N4O4S
• Molecular Weight: 535.44
• Purity: ≥95%
• Synonyms: N-[4-[[4-[2-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]propan-2-yl]phenoxy]methyl]pyrimidin-2-yl]methanesulfonamide
• InChI: InChI=1S/C24H24Cl2N4O4S/c1-24(2,18-12-16(14-27)22(21(26)13-18)33-11-9-25)17-4-6-20(7-5-17)34-15-19-8-10-28-23(29-19)30-35(3,31)32/h4-8,10,12-13H,9,11,15H2,1-3H3,(H,28,29,30)
• InChIKey: GVCZSODXLFBYSS-UHFFFAOYSA-N
• SMILES: CC(C)(C1=CC=C(C=C1)OCC2=NC(=NC=C2)NS(=O)(=O)C)C3=CC(=C(C(=C3)Cl)OCCCl)C#N

Masofaniten (Androgen receptor-IN-2) is a potent and orally active androgen receptor inhibitor. Masofaniten has antitumor activity against prostate cancer[1].
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].
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].

Reference

[1]. Han-Jie Zhou, et al. Androgen receptor modulators and methods for their use. Patent. US20200123117A1.