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2-hydroxy Flutamide

 
Catalog No.
C4721
雄激素受体抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,570.00
Ship with 10-15 days
10mg
¥ 2,275.00
Ship with 10-15 days
25mg
¥ 3,737.00
Ship with 10-15 days
50mg
¥ 5,308.00
Ship with 10-15 days

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背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt292.2
Cas No.52806-53-8
FormulaC11H11F3N2O4
SynonymsHydroxyniphtholide,SCH 16423
Solubility≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide
Chemical Name2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide
SDFDownload SDF
Canonical SMILESO=C(C(O)(C)C)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1
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质量控制

Quality Control & MSDS

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Chemical structure

2-hydroxy Flutamide