13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:Bicalutamide
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 100mg |
| CAS | 9 |
| 別名 | N/A |
| 化學名 | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide |
| 分子式 | C18H14F4N2O4S |
| 分子量 | 430.37 |
| 溶解度 | ≥ 21.5mg/mL in DMSO, ≥ 4.3 mg/mL in EtOH with ultrasonic |
| 儲存條件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
Bicalutamide is an active non-steroidal androgen receptor antagonist with IC50 value of 160 nM.[1]
The androgen receptor (AR) is a type of nuclear receptor. It is activated by binding of either of dihydrotestosterone or the androgenic hormones testosterone. Then, it will translocate into the nucleus as DNA-binding transcription factor which regulates gene expression. Androgen is critical for the maintenance and development of the male sexual phenotype through related gene. The androgen receptor (AR) is also related to the core mechanism of castration-resistant prostate cancer.[1]
Bicalutamide inhibits growth in prostate cancer cells (VCaP cells) which overexpress androgen receptor by directly binding to AR then mediates androgen-mediated gene transcription with IC50 value of 160 nM. Bicalutamide directly binds to androgen receptor with Ki value of 12.5μM. In prostate cancer cells, bicalutamide impairs DNA binding and nuclear localization. Bicalutamide and MDV3100 significantly inhibited R1881-induced VP16-AR–mediated transcription in HepG2 cells with an IC50 value of 0.2 μM.[1] Bicalutamide has been an molecular template for designing selective androgen receptor antagonist used to the treatment of prostate cancer cells.[2] Bicalutamide also induces cell death by a different pathway which is independent of mitochondrial membrane potential changes and Bcl-2 action.[1]
Bicalutamide significantly inhibited AR then decrease the tumor growth in murine xenograft models, male immunodeficient mice which harbors LNCaP/AR-luc xenograft tumors.[1]
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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