RD162 是一种与雄激素受体 (AR) 特异性结合的非甾体抗雄激素 (NSAA)。

RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).

RD162 has little to no binding to the progesterone, estrogen, or glucocorticoid receptors. RD162 (1-10 μM) suppressed growth and induces apoptosis in the human prostate cancer cell line VCaP which had endogenous AR gene amplification[1].

RD162 (20 mg/kg) is ~50 percent bioavailable after oral delivery with a serum half-life of about 30 hours. RD162 (10 mg/kg; oral gavage) causes all tumors regressed. RD162 (0.1, 1, 10 mg/kg; oral gavage) consistently reduces luciferase activity with 10 mg/kg/day human LNCaP/AR xenografts grown in castrated male mice whereas lower doses of 0.1 and 1.0 mg/kg/day has minimal effect. RD162 substantially reduces cellular proliferation after 5 days[1].

915087-27-3

C22H16F4N4O2S

476.45

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years