| 2-hydroxy Flutamideandrogen receptor inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 52806-53-8 | SDF | Download 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 |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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尤其是获得SCI文献引用的产品，
绝对ok的
我想用酶联免疫斑点（ELISPOT）技术测定NK细胞活性，但不知道哪里能买到试剂盒，特向大家求助，谢谢。
