产品
编 号：F580272
分子式：C22H16F4N4O2S
分子量：476.45
分子式：C22H16F4N4O2S
分子量：476.45
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 915087-27-3
产品详情
生物活性：
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
体内研究：
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 xenografts
Dosage:10 mg/kg
Administration:Oral gavage; daily; for 28 days
Result:Caused all tumors regressed.
Animal Model:Male mice
Dosage: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.
体外研究：
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.
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
体内研究：
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 xenografts
Dosage:10 mg/kg
Administration:Oral gavage; daily; for 28 days
Result:Caused all tumors regressed.
Animal Model:Male mice
Dosage: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.
体外研究：
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.
产品资料
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