- ARN-509
- RU 58841
- Andarine
- MDV3100 (Enzalutamide)
- 17 alpha-propionate
- Spironolactone
| BicalutamideAndrogen receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 99.46%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
Related Biological Data
| Cell experiment [1]: | |
Cell lines | VCaP or Hep-G2 cell lines |
Preparation method | The solubility of this compound in DMSO is >21.5 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 10-11 -10-4 M |
Applications | Bicalutamide was found to be able to inhibit the growth in prostate cancer cells (VCaP cells) with overexpressed androgen receptor through directly binding to AR then mediating androgen-mediated gene transcription. Moreover, bicalutamide could impair the DNA binding and nuclear localization in prostate cancer cells. In HepG2 cells, bicalutamide could also significantly inhibit R1881-induced VP16-AR–mediated transcription with an IC50 value of 0.2 μM. |
| Animal experiment [1]: | |
Animal models | Male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors |
Dosage form | 10 mg/kg/day, oral |
Application | In a clinically valid murine xenograft model of human CRPC, bicalutamide showed greater efficacy than MDV3100. Maximal therapeutic response in this model was achieved at 30 mg/kg/d of bicalutamide, whereas the same response required 100 mg/kg/d of MDV3100 and higher steady-state plasma concentrations. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L et al: ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res 2012, 72(6):1494-1503. | |
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| Cas No. | 90357-06-5 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 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 | ||
| Formula | C18H14F4N2O4S | M.Wt | 430.37 |
| Solubility | ≥21.5mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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]References: [1]. Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L et al: ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res 2012, 72(6):1494-1503.[2]. Yin D, He Y, Perera MA, Hong SS, Marhefka C, Stourman N, Kirkovsky L, Miller DD, Dalton JT: Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. Mol Pharmacol 2003, 63(1):211-223.
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说得简单点就是，细胞核是原封不动的，没有重组过，而细胞核外的东西是很多别的细胞中提取出来的并组合起来的。这样的混合体淋巴细胞产生的抗体具有很强的嵌合能力，针对性比一般的抗体强，但是它的来源没变，所以称之为混合单克隆抗体
制备抗体都需要进行纯化处理
清冷冻干燥后保存。
没有marker，怎么知道你做的蛋白大小？
没有参照物，怎么知道你跑的快不快？
没有尺子，怎么知道你的size大小？
凭嘴说吗？
单克隆抗体这项新技术从根本上解决了在抗体制备中长期存在的特异性和可重复性问题，可用于探讨: ①蛋白质的精细结构；②淋巴细胞亚群的表面新抗原；③组织相容性抗原；④激素和药物的放射免疫（或酶免疫）分析；⑤肿瘤的定位和分类；⑥纯化微生物和寄生虫抗原；⑦免疫治疗和与药物结合的免疫-化学疗法 (“导弹”疗法,利用单克隆抗体与靶细胞特异性结合，将药物带至病灶部位.。
因此，单克隆抗体可直接用于人类疾病的诊断、预防、治疗以及免疫机制的研究，为人类恶性肿瘤的免疫诊断与免疫治疗开辟了广阔前景。
