氟他胺, 雄激素受体拮抗剂

Androgen Receptor Antagonists
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
F408131-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 SCH-13521 | 2-​methyl-​N-​[4-​nitro-​3-​(trifluoromethyl)​phenyl]​-propanamide
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Flutamide
生化机理 氟他胺(SCH-13521)是一种抗雄激素药物,其活性代谢物与雄激素受体结合的Ki值为 55 nM,主要用于治疗前列腺癌。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 雄激素受体拮抗剂
产品介绍

Flutamide is an androgen receptor inhibitor with chemopreventive properties against bladder and prostate carcinogenesis. Flutamide inhibits the expression of testosterone regulated transforming growth factor β-1 (TGF-β1).An androgen receptor antagonist

Information

Flutamide Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with K i values of 55 nM, and primarily used to treat prostate cancer.
In vitro

Flutamide (Eulexin) is an antiandrogen drug. Flutamide-OH, the active metabolite of flutamide, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM. Flutamide does not affect the proliferation of an androgen-sensitive clone of the mouse mammary carcinoma Shionogi SC-l 15 cells in culture, shows only antiandrogenic effect, but not androgenic effect. Flutamide provides treatment for prostate cancer when used along with leuprolide.

In vivo

Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of flutamide and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity.
Cell Data

cell lines:

Concentrations:~1 μM

Incubation Time:40 days

Powder Purity:≥99%

产品属性

ALogP 2.916
hba_count 1
HBD Count 1
Rotatable Bond 4

关联靶点(人)

CYP1A2 Tchem 细胞色素 P450 1A2(Cytochrome P450 1A2) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AR Tclin 雄激素受体(Androgen receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
AADAC Tchem 芳基乙酰胺脱乙酰酶(Arylacetamide deacetylase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CC(C)C(=O)NC1=CC(=C(C=C1)[N+]([O-])=O)C(F)(F)F
分子量 276.21
Reaxy-Rn 2157663
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2157663&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 55
DMSO(mM) Max Solubility 199.12
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 2157663
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2157663&ln=

技术规格说明书

Concentration(Compounding value) 9.0-11.0(mmol/L)
Proton NMR spectrum Conforms to Structure
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

1. Jiao Sha, Kaibo Hu, Tingting Li, Zidan Cao, Yameng Wan, Renren Sun, Haixia He, Gaoliang Jiang, Yu Li, Tao Li, Baozeng Ren.  (2021)  Solubility determination, model correlation, solvent effect, molecular simulation and thermodynamic properties of flutamide in eleven pure solvents at different temperatures.  JOURNAL OF MOLECULAR LIQUIDS,  336  (115559).  [10.1016/j.molliq.2021.115559]

参考文献

1. Jiao Sha, Kaibo Hu, Tingting Li, Zidan Cao, Yameng Wan, Renren Sun, Haixia He, Gaoliang Jiang, Yu Li, Tao Li, Baozeng Ren.  (2021)  Solubility determination, model correlation, solvent effect, molecular simulation and thermodynamic properties of flutamide in eleven pure solvents at different temperatures.  JOURNAL OF MOLECULAR LIQUIDS,  336  (115559).  [10.1016/j.molliq.2021.115559]

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