| 产品描述: | 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 |
| 靶点: |
AndrogenReceptor |
| 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. Cell Viability Assay Cell Line: VCaP cells Concentration: 1, 10 μM Incubation Time: 4 days Result: Suppressed cell growth. |
| 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. |
| 参考文献: |
1. Chris Tran, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90. |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.099 ml |
10.494 ml |
20.989 ml |
| 5 mM |
0.42 ml |
2.099 ml |
4.198 ml |
| 10 mM |
0.21 ml |
1.049 ml |
2.099 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.42 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |