2-hydroxy Flutamide
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 292.2 |
Cas No. | 52806-53-8 |
Formula | C11H11F3N2O4 |
Synonyms | Hydroxyniphtholide,SCH 16423 |
Solubility | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
Chemical Name | 2-hydroxy-2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]-propanamide |
SDF | Download SDF |
Canonical SMILES | O=C(C(O)(C)C)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)