Androgen receptor-IN-2
Names
[ CAS No. ]:
2416716-62-4
[ Name ]:
Androgen receptor-IN-2
Biological Activity
[Description]:
Androgen receptor-IN-2 is a potent and orally active Androgen Receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer[1].
[Related Catalog]:
[Target]
Androgen receptor[1]
[In Vitro]
Androgen receptor-IN-2 (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC50 of 535 nM[1]. Androgen receptor-IN-2 inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively)[1]. Androgen receptor-IN-2 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]
Androgen receptor-IN-2 (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors[1]. Androgen receptor-IN-2 (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: LNCaP Xenografts Model[1] Dosage: 60 mg/kg Administration: Oral administration (p.o.) Result: Inhibited tumor growth no obvious drug related toxicity (bodyweight change).
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C24H24Cl2N4O4S
[ Molecular Weight ]:
535.44