2-hydroxy Flutamide
(Synonyms: 羟基氟他胺,Hydroxyniphtholide,SCH 16423) 目录号 : GC17160
An active metabolite of the antiandrogen flutamide
Cas No.:52806-53-8
Sample solution is provided at 25 µL, 10mM.
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2-hydroxyFlutamide is an androgen receptor (AR) inhibitor [1].
The androgen receptor has been implicated in the development and progression of prostate cancer. AR is expressed in many androgen-independent or hormone refractory prostate cancers and is maintained throughout prostate cancer progression. Inactivation of AR may delay prostate cancer progression [2].
2-hydroxyFlutamide is the major metabolite of flutamide generated during the metabolism of the non-steroidal antiandrogen flutamide by CYP1A2 and CYP3A4. Flutamide is an antiandrogenic drug which has been widely used for treatment of prostate cancer. 2-hydroxyflutamide could inhibit flutamide metabolism. In cells, increased conversion of flutamide to 2-hydroxyflutamide or accumulation of 2-hydroxyflutamide may result in the anomalous responses to flutamide, which can be observed in some advanced prostate cancers [3]. 2-hydroxy flutamide blocked the expression of AR target genes and prevented androgen-dependent stabilization of the AR [1]. 2-hydroxyFlutamide was a more powerful antiandrogen in vivo, with higher binding affinity for the AR than flutamide. In humans, hydroxyflutamide exhibited an elimination halflife of about 8 h [3].
References:
[1] Kolvenbag G, Furr B J A, Blackledge G R P. Receptor affinity and potency of non-steroidal antiandrogens: translation of preclinical findings into clinical activity[J]. Prostate cancer and prostatic diseases, 1998, 1: 307-314.
[2] Heinlein C A, Chang C. Androgen receptor in prostate cancer[J]. Endocrine reviews, 2004, 25(2): 276-308.
[3] Shet M S, McPhaul M, Fisher C W, et al. Metabolism of the antiandrogenic drug (Flutamide) by human CYP1A2[J]. Drug metabolism and disposition, 1997, 25(11): 1298-1303.
[4] Gao W, Kim J, Dalton J T. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands[J]. Pharmaceutical research, 2006, 23(8): 1641-1658.
| Cas No. | 52806-53-8 | SDF | |
| 别名 | 羟基氟他胺,Hydroxyniphtholide,SCH 16423 | ||
| 化学名 | 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide | ||
| Canonical SMILES | O=C(C(O)(C)C)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 | ||
| 分子式 | C11H11F3N2O4 | 分子量 | 292.2 |
| 溶解度 | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4223 mL | 17.1116 mL | 34.2231 mL |
| 5 mM | 0.6845 mL | 3.4223 mL | 6.8446 mL |
| 10 mM | 0.3422 mL | 1.7112 mL | 3.4223 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