RD162

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RD162 是第二代口服抗雄激素，可与雄激素受体 (AR) 结合，IC50 为 30.9 nM。

RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM; suppresses growth and induces apoptosis in human prostate cancer cells in vitro, demonstrates greater relative affinity than the clinically used antiandrogen bicalutamide, reduces the efficiency of its nuclear translocation, and impairs both DNA binding to androgen response elements and recruitment of coactivators; induces tumor regression in mouse models of castration-resistant human prostate cancer.

RD162 (1-10 μM; 4 days) suppresses growth and induces apoptosis in the human prostate cancer cell line VCaP which has endogenous AR gene amplification. RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay. Cell Viability AssayCell Line:VCaP cells Concentration:1, 10 μM Incubation Time:4 daysResult:Suppressed cell growth.

RD162 (10 mg/kg; oral gavage; daily; for 28 days) causes all tumors regressed. RD162 (0.1, 1, 10 mg/kg; oral gavage; daily; for 5 days) 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. RD162 (20 mg/kg; gavage) is ～50 percent bioavailable after oral delivery with a serum half-life of about 30 hours. Animal Model:Castrate male mice bearing LNCaP/AR xenograftsDosage:10 mg/kg Administration:Oral gavage; daily; for 28 days Result:Caused all tumors regressed.Animal Model:Male miceDosage:20 mg/kg (Pharmacokinetic Analysis) Administration:Oral gavage (in 0.5% hydroxy-methyl-propyl-cellulose)Result:Had ～50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.

RD 162 | RD-162

Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor (AR)

Neurological Disease

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915087-27-3

476.45

C22H16F4N4O2S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (262.36 mM)

CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CC(=C(C=C4)C#N)C(F)(F)F)F

4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-benzamide

(-20℃)

With Ice Pack

≥ 2 years