Androgen receptor-IN-2 is a potent and orally active androgen receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer.
性状
Solid
IC50 & Target[1][2]
Androgen receptor
体外研究(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.Androgen receptor-IN-2 inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively).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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
Androgen receptor-IN-2 (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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Han-Jie Zhou, et al. Androgen receptor modulators and methods for their use. Patent. US20200123117A1.
溶解度数据
In Vitro: DMSO : 50 mg/mL (93.38 mM; Need ultrasonic and warming)配制储备液