Nilutamide
(Synonyms: 尼鲁米特,Nilandron; RU 23908) 目录号 : GC44405
A non-steroidal androgen receptor antagonist
Cas No.:63612-50-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nilutamide is a non-steroidal antiandrogen that is an antagonist of the androgen receptor. It reverses testosterone-induced increases in cell proliferation with an IC50 value of 412 nM in mouse mammary carcinoma cells in vitro. It has antiandrogenic activity in both intact and castrated rats, inhibiting testosterone propionate-induced prostate growth when administered at a dose of 2.5 mg/kg. Formulations containing nilutamide have been used in combination with surgical castration in the treatment of metastatic prostate cancer.
| Cas No. | 63612-50-0 | SDF | |
| 别名 | 尼鲁米特,Nilandron; RU 23908 | ||
| Canonical SMILES | O=C1N(C2=CC(C(F)(F)F)=C([N+]([O-])=O)C=C2)C(C(C)(C)N1)=O | ||
| 分子式 | C12H10F3N3O4 | 分子量 | 317.2 |
| 溶解度 | Chloroform: slightly soluble,DMSO: 25mM,Ethanol: 25mM,Methanol: slightly soluble | 储存条件 | Store at -20°C |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1526 mL | 15.7629 mL | 31.5259 mL |
| 5 mM | 0.6305 mL | 3.1526 mL | 6.3052 mL |
| 10 mM | 0.3153 mL | 1.5763 mL | 3.1526 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。
Nilutamide: an antiandrogen for the treatment of prostate cancer
Ann Pharmacother 1997 Jan;31(1):65-75.PMID:8997470DOI:10.1177/106002809703100112.
Objective: To review the pharmacology, pharmacokinetics, efficacy, and adverse effects of Nilutamide and to compare this agent with the currently marketed nonsteroidal antiandrogens (i.e., bicalutamide, flutamide) by critically analyzing the published literature. Data sources: MEDLINE (1980-1995) and CANCERLIT (1991-1995) were searched for English-language publications using the terms Nilutamide, bicalutamide, and flutamide alone, and either Nilutamide or androgen antagonists in combination with prostatic neoplasms. Study selection and data extraction: All articles with subject matter on Nilutamide, bicalutamide, and flutamide were considered for inclusion. For studies published in more than one journal, the first publication was used unless a subsequent publication included additional or follow-up data, in which case the latter publication was cited instead. Data synthesis: Nilutamide was effective in combination with orchiectomy in improving responses in patients with advanced prostate cancer. However, patient survival was not improved in these trials, and improvements in bone pain did not usually result in improved performance status in these patients. The few trials of Nilutamide monotherapy or Nilutamide in combination with a luteinizing hormone-releasing hormone analog are too small to draw meaningful conclusions regarding its efficacy or its role in the treatment of advanced prostate cancer. No comparative trials of Nilutamide with other antiandrogens and no analysis of the impact of Nilutamide on patient quality of life are currently available. Nilutamide appears to produce a higher frequency of adverse effects than the other currently marketed nonsteroidal antiandrogens, bicalutamide and flutamide. Conclusions: Nilutamide does not appear to represent a major advance in the treatment of advanced prostate cancer and appears to be somewhat inferior to both flutamide and bicalutamide with regard to adverse effects. Nilutamide should not be considered the antiandrogen of choice in the treatment of advanced prostate cancer.
Nilutamide
Acta Crystallogr Sect E Struct Rep Online 2012 Mar 1;68(Pt 3):o591.PMID:22412506DOI:10.1107/S1600536812003728.
THE CRYSTAL STRUCTURE OF Nilutamide [SYSTEMATIC NAME: 5,5-dimethyl-3-[4-nitro-3-(trifluoro-meth-yl)phen-yl]imidazolidine-2,4-dione], C(12)H(10)F(3)N(3)O(4), was determined at 150 K. The dihedral angle between the mean planes through the imidazoline [maximum deviation = 0.0396 (14) Å] and benzene rings is 51.49 (5)°. The mol-ecule exhibits inter-molecular hydrogen bonding via N-H⋯O inter-actions, resulting in the formation of chains parallel to the c axis.
Nilutamide. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in prostate cancer
Drugs Aging 1993 Jan-Feb;3(1):9-25.PMID:8453188DOI:10.2165/00002512-199303010-00002.
Nilutamide is a nonsteroidal antiandrogen with affinity for androgen receptors but not for progestogen, estrogen, or glucocorticoid receptors. Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and cancerous prostatic tissue. Nilutamide has a long half-life which permits once-daily administration. Nilutamide is usually given in combination with surgical or chemical castration using gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH)] agonists. In castrated patients the addition of Nilutamide improves objective response rates, bone pain, urinary symptoms, tumour markers and time to disease progression. The tolerance of Nilutamide is generally acceptable. Adverse effects are usually mild and reversible and consistent with androgen depletion. Unexpected but reversible adverse effects of Nilutamide include delayed adaption to dark after exposure to bright light, transient increases in transaminases, and more severe but rare interstitial pneumonitis. Thus, Nilutamide is a welcome treatment option that may be particularly useful in patients to whom the convenience of once-daily administration is seen as a worthwhile benefit.
Pharmacokinetics and metabolism of Nilutamide
Urology 1991;37(2 Suppl):13-9.PMID:1992598DOI:10.1016/0090-4295(91)80096-p.
Data are available on the pharmacokinetics and metabolism of Nilutamide in the rat, dog, and human (normal volunteers and patients with advanced prostatic carcinoma). Studies using 14Carbon-nilutamide, radioimmunoassay, and high-performance liquid chromatography (HPLC) are reviewed. In the rat, bioavailability by the oral route was complete. The majority of the plasma radioactivity was unchanged Nilutamide up to six hours, t1/2 was seven hours, and clearance was 150 mL/hour/kg body weight. Metabolism studies identified 6 urinary metabolites. The major metabolites result from reduction of the nitro group initially to an hydroxylamine (17%) and then to a primary amino (26%) group. In normal volunteers the compound was rapidly absorbed, displayed linear kinetics over a dose range of 100-300 mg, and declined slowly in plasma with a terminal phase t1/2 of forty-three to forty-nine hours. In studies in 12 patients with advanced (Stage D) prostatic carcinoma, single-dose kinetics after 14C-nilutamide and kinetics with repetitive twice-daily dosing of two to seven weeks were measured. Terminal phase plasma t1/2 of unchanged Nilutamide was 56 +/- 19 hours and of total radioactivity 87 +/- 27 hours (mean +/- SD). Area under the curve of plasma radioactivity was 23 to 38 percent unchanged Nilutamide. Urinary excretion of radioactivity was slow and incomplete because the collection time was not long enough in regard to t1/2 (mean after 5 days, 62 +/- 10%) and consisted almost entirely of metabolites. Steady-state plasma levels of Nilutamide were reached in about two weeks. It can be concluded that in humans, unlike other species, plasma decay of Nilutamide is very slow. Elimination is almost exclusively by metabolism. Single-daily dosing is appropriate. Hepatic impairment could be expected to prolong plasma decay; renal impairment is likely to have little effect.
Castration plus Nilutamide vs castration plus placebo in advanced prostate cancer. A review
Urology 1991;37(2 Suppl):20-4.PMID:1992599DOI:10.1016/0090-4295(91)80097-q.
Combination of antiandrogen treatment with surgical or medical castration should improve the efficacy of endocrine treatment of prostatic cancer by blocking the effects of adrenal androgens. A nonsteroidal antiandrogen, Nilutamide, has shown promising results in preliminary open studies. In a short-term (29 days) comparison of Nilutamide plus buserelin and buserelin plus placebo, Nilutamide (300 mg/day), significantly reduced bone pain, and fewer patients experienced worsening pain than in the control group. The initial buserelin-induced increase in prostatic acid phosphatase was prevented by Nilutamide, but there was a similar increase in testosterone and gonadotropin concentrations to that seen in the control group. Thus, Nilutamide can prevent the tumor flare-up associated with the start of luteinizing hormone-releasing hormone (LH-RH) treatment, even though the endocrine responses are not affected. In three multicenter, randomized, double-blind placebo-controlled trials of castration and Nilutamide involving 248 patients, the combination of Nilutamide and castration decreased bone pain, improved performance status, and increased the number of patients with objective regression, compared with patients who were castrated but did not receive Nilutamide. Nilutamide was generally well tolerated, though visual disorders, gastrointestinal disorders, and alcohol intolerance were reported in patients receiving Nilutamide. The results suggest that Nilutamide improves the efficacy of castration in patients with prostatic cancer. Current studies are investigating the effects of this treatment on survival and the risk-benefit ratio.