Bicalutamide
(Synonyms: 比卡鲁胺) 目录号 : GC12271
Bicalutamide是一种非甾体抗雄激素药物，可通过选择性和竞争性地阻断雄激素与雄激素受体（AR）的结合，在外周组织中发挥抗雄激素作用。
Cas No.:90357-06-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Bicalutamide is a non-steroidal antiandrogen that selectively and competitively blocks androgen binding to the androgen receptor (AR), exerting anti-androgenic effects in peripheral tissues[1-2]. Bicalutamide is used for the treatment of advanced prostate cancer[3].
In vitro, after VCaP cells were treated for 7 days with increasing concentrations of Bicalutamide (10-10-10-5mol/L), Bicalutamide dose-dependently promoted cell proliferation and partially antagonized the effect of the synthetic androgen R1881[4]. Treatment of mature dendritic cells (mDCs) with 20μM Bicalutamide for 24h induced a modest but significant up-regulation of CD86 and HLA-DR, down-regulated CD11c, and markedly reduced both transforming growth factor-β (TGF-β) and interleukin-10 (IL-10) protein levels[5].
In vivo, in male BALB/c mice, daily intraperitoneal injection of 0.02mg Bicalutamide in 0.5ml saline for 7 consecutive days significantly reduced eosinophil infiltration in the nasal mucosa, markedly lowered serum levels of IgE, IL-4, and IL-6, and substantially decreased the surface expression of histamine receptors on mast cells, while also markedly suppressing p-protein kinase B (p-PKB) and mTOR protein levels in these cells[6]. In knock-in spinal and bulbar muscular atrophy (SBMA) (KI AR113Q) mice given twice-weekly subcutaneous Bicalutamide (2mg/kg in 50µL corn oil), the drug reversed muscle AR insoluble aggregate formation, restored autophagic flux, and suppressed apoptosis, yielding partial recovery of muscle morphology and function, improved motor performance, and prolonged survival[7].
References:
[1] Carvalho RM, Santos LDN, Ramos PM, et al. Bicalutamide and the new perspectives for female pattern hair loss treatment: What dermatologists should know. J Cosmet Dermatol. 2022;21(10):4171-4175.
[2] Aulakh S, Mysore V. Bicalutamide: A review. J Cutan Aesthet Surg. 2025;18(2):78-85.
[3] Kolvenbag GJ, Blackledge GR. Worldwide activity and safety of bicalutamide: a summary review. Urology. 1996;47(1A Suppl):70-84.
[4] Clegg NJ, Wongvipat J, Joseph JD, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012;72(6):1494-1503.
[5] Nourbakhsh NS, Naeimi S, Moghanibashi M, et al. Bicalutamide reveals immunomodulatory effects in prostate cancer by regulating immunogenic dendritic cell maturation. Tissue Cell. 2024;91:102530.
[6] Zhang Y, Zhang Q, Wu X, et al. Bicalutamide, an androgen receptor antagonist, effectively alleviate allergic rhinitis via suppression of PI3K-PKB activity. Eur Arch Otorhinolaryngol. 2023;280(2):703-711.
[7] Galbiati M, Meroni M, Boido M, et al. Bicalutamide and Trehalose Ameliorate Spinal and Bulbar Muscular Atrophy Pathology in Mice. Neurotherapeutics. 2023;20(2):524-545.
Bicalutamide是一种非甾体抗雄激素药物，可通过选择性和竞争性地阻断雄激素与雄激素受体（AR）的结合，在外周组织中发挥抗雄激素作用[1-2]。Bicalutamide用于治疗晚期前列腺癌[3]。
在体外，将VCaP细胞用递增浓度的Bicalutamide（10-10-10-5mol/L）处理7天后，Bicalutamide呈剂量依赖性促进细胞增殖，并可部分拮抗合成雄激素R1881的作用[4]。用20μM的Bicalutamide处理成熟树突状细胞（mDCs）24小时，可温和但显著地上调CD86和HLA-DR表达，下调CD11c，并显著降低转化生长因子-β（TGF-β）和白细胞介素-10（IL-10）蛋白水平[5]。
在体内，对雄性BALB/c小鼠每日腹腔注射0.02mg的Bicalutamide（溶于0.5ml生理盐水），连续7天，可显著减少鼻黏膜嗜酸性粒细胞浸润，显著降低血清IgE、IL-4和IL-6的水平，并显著抑制肥大细胞表面组胺受体的表达，同时显著下调肥大细胞内p-蛋白激酶B（p-PKB）和mTOR蛋白水平[6]。在敲入脊髓延髓肌萎缩症（SBMA）KI AR113Q小鼠中，每周两次皮下注射Bicalutamide（2mg/kg，溶于50µL玉米油），可逆转肌肉内AR不溶性聚集体形成、恢复自噬通量、抑制凋亡，从而部分恢复肌肉形态与功能，改善运动表现并延长生存期[7]。
| Cell experiment [1]: | |
Cell lines | Mature dendritic cells (mDCs) |
Preparation Method | A total of 3×105 cells were cultured in four wells of a 24-well plate. Cells were exposed to 20μM Bicalutamide. The plate was then incubated at 37°C for 24 hours. After the incubation period, the surface expression of markers associated with mDCs and antigen presentation were assessed to conduct the phenotypic characterization of both mDCs and Bicalutamide-treated mDCs. |
Reaction Conditions | 20μM; 24h |
Applications | Flow cytometry results demonstrated a slightly significant upregulation of CD86 and HLA-DR in the mDC + Bicalutamide group compared to the mDC group. However, CD11c expression was downregulated in mDC + Bicalutamide. Following the treatment of mDCs with Bicalutamide, the expression levels of Transforming growth factor-β (TGF-β) and Interleukin-10 (IL-10) in the Bicalutamide-mDC group exhibited a significant decrease compared to mDCs. |
| Animal experiment [2]: | |
Animal models | Male KI AR113Q mice |
Preparation Method | To analyze the effects of Bicalutamide and trehalose on knock-in spinal and bulbar muscular atrophy (SBMA) (KI AR113Q) mice, we administered: Bicalutamide by subcutaneous injection (50μL, 2mg/kg, dissolved in corn oil) twice a week from 6 weeks of age until death or sacrifice (max 52 weeks). In a second experiment, animals were treated with Bicalutamide from 12 weeks of age and sacrificed at 26 weeks of age. We analyzed: mouse survival curves, motor behavior (once a week), and molecular changes in the spinal cord and gastrocnemius muscle. |
Dosage form | 2mg/kg; subcutaneous injection |
Applications | Bicalutamide achieves much lower concentrations in the central nervous system (CNS) than in plasma. In KI AR113Q mice, Bicalutamide reversed the formation of androgen receptor (AR) insoluble forms in muscle and prevented the blockage of autophagic flux. Bicalutamide also blocked the activation of apoptosis that occurs in KI AR113Q muscle. Bicalutamide led to a partial recovery of muscle morphology and function, improved the motor performance of SBMA mice, and extended their survival. |
References: | |
| Cas No. | 90357-06-5 | SDF | |
| 别名 | 比卡鲁胺 | ||
| 化学名 | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide | ||
| Canonical SMILES | CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O | ||
| 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 | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3236 mL | 11.6179 mL | 23.2358 mL |
| 5 mM | 0.4647 mL | 2.3236 mL | 4.6472 mL |
| 10 mM | 0.2324 mL | 1.1618 mL | 2.3236 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet