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2-hydroxy Flutamide (Synonyms: Hydroxyniphtholide,SCH 16423)

Catalog No.GC17160

2-hydroxy Flutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC50=700 nM). 2-hydroxy Flutamide can be used for the research of prostate cancer.

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2-hydroxy Flutamide Chemical Structure

Cas No.: 52806-53-8

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Sample solution is provided at 25 µL, 10mM.

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Background

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.

Chemical Properties

Cas No. 52806-53-8 SDF
Synonyms Hydroxyniphtholide,SCH 16423
Chemical Name 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
Formula C11H11F3N2O4 M.Wt 292.2
Solubility ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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