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2-hydroxy Flutamide
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
2-hydroxy Flutamide图片
CAS NO:52806-53-8
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
2-hydroxy Flutamide (HF) 是 Flutamide 的活性代谢物，是一种有效的雄激素受体拮抗剂 (IC50=700 nM)。 2-羟基氟他胺可用于前列腺癌的研究。
Cas No.52806-53-8
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 SMILESO=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℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.