货号:A208282
同义名:
SCH 13521; Niftolide
Flutamide是一种非甾体类雄激素受体(AR)拮抗剂,通过竞争性结合雄激素受体,阻断睾酮和二氢睾酮(DHT)的作用,从而抑制前列腺癌细胞的生长。其活性代谢物2-羟基氟他胺具有更高的AR亲和力,常用于研究前列腺癌,特别是在与GnRH类似物联合使用时效果显著。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM |
98% | |||||||||||||||||
| Apalutamide |
+++
Androgen Receptor, IC50: 16 nM |
98% | |||||||||||||||||
| AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM |
99% | |||||||||||||||||
| Darolutamide |
++++
Androgen receptor, Ki: 11 nM |
98% | |||||||||||||||||
| Flutamide |
+++
Androgen Receptor, Ki: 55 nM |
98% | |||||||||||||||||
| Galeterone |
++
Androgen Receptor, IC50: 384 nM |
98% | |||||||||||||||||
| Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM |
98% | |||||||||||||||||
| Megestrol | ✔ | 98% | |||||||||||||||||
| Spironolactone |
++
Androgen Receptor, IC50: 77 nM |
98+% | |||||||||||||||||
| Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM |
99% | |||||||||||||||||
| EPI-001 |
+
Androgen Receptor, IC50: ~6 μM |
98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. Flutamide, mainly used in the treatment of prostate cancer, is an antiandrogenic drug. Flutamida-OH is the active metabolite form of Flutamide and directly binds to the androgen receptor with Ki of 55 nM. In rat adenohypophysial cells in primary culture, the specific uptake of [3H] testosterone (T) is completely blocked by increasing concentrations of the pure antiandrogen flutamide-OH at an IC50 value of 50 nM [8]. In adult male rats, Treatment for 10 days with flutamide (5 mg/rat, twice daily) caused a marked stimulation of plasma testosterone (T) associated with a significant increase in plasma gonadotropin concentrations and inhibited plasma prolactin (PRL) levels. Moreover, flutamide treatment alone produces an important inhibition of ventral prostate and seminal vesicle weights associated with a significant decrease in prostatic beta-adrenergic receptor levels [9]. |
| Concentration | Treated Time | Description | References | |
| HepG2 cells | 0.05–300 µM | 2 hours | To compare the mitochondrial toxicity of flutamide, 2-hydroxyflutamide, and bicalutamide in glucose or galactose-conditioned cells. Flutamide and 2-hydroxyflutamide significantly reduced ATP content in galactose medium, indicating mitochondrial toxicity. | Toxicol Sci. 2016 Oct;153(2):341-51. |
| Mouse primary hepatocytes | 10 µM or 50 µM | 24 hours | FLU elevated Cyp1a1, Cyp1a2, Cyp1b1, Nqo1, and Gsta1 mRNA levels at both 10 and 50 μM, indicating that FLU directly activates the AhR signaling pathway. | Biochem Pharmacol. 2016 Nov 1;119:93-104. |
| HepG2 cells | 5 µM, 20 µM, and 100 µM | 24 hours | FLU significantly increased AhR-dependent luciferase activity at 5 μM and higher concentrations, indicating that FLU can activate AhR. | Biochem Pharmacol. 2016 Nov 1;119:93-104. |
| Hepa-1c1c7 cells | 5 µM, 20 µM, and 100 µM | 24 hours | FLU significantly increased AhR-dependent luciferase activity at 5 μM and higher concentrations, indicating that FLU can activate AhR. | Biochem Pharmacol. 2016 Nov 1;119:93-104. |
| Human keratinocytes (HaCaT) | 5 mg/ml | 72 hours | To investigate the effect of Flutamide on HaCaT cell proliferation, results showed that F-PCL and DF-PCL scaffolds significantly increased HaCaT cell proliferation. | FASEB J. 2022 May;36(5):e22310. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6N | C57BL/6N mice | Gavage | 200 mg/kg | Once daily for 28 days | After 28 days of FLU treatment, a significant increase in liver weights and liver/body weight ratios was observed, along with elevated bile acid levels in serum and liver, indicating that FLU induced hepatomegaly and disrupted bile acid homeostasis. | Biochem Pharmacol. 2016 Nov 1;119:93-104. |
| BALB/C mice | Severe burn wound healing model | Topical administration | 5 mg/ml | Single administration, lasting 28 days | To investigate the effect of Flutamide on burn wound healing in mice, results showed that F-PCL scaffolds significantly accelerated wound healing, and DF-PCL scaffolds further promoted wound healing. | FASEB J. 2022 May;36(5):e22310. |
| Dose | Mice: 6.6 mg/kg, 33 mg/kg[3] (s.c.); 60 mg/kg[4] (i.p.) Rat: 50 mg/kg - 200 mg/kg[5] (p.o.); 12 mg/kg[6] (i.v.) | ||||||||||||||||||||
| Administration | s.c., i.p. | ||||||||||||||||||||
| Pharmacokinetics |
|
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.62mL 0.72mL 0.36mL |
18.10mL 3.62mL 1.81mL |
36.20mL 7.24mL 3.62mL |
|
| CAS号 | 13311-84-7 |
| 分子式 | C11H11F3N2O3 |
| 分子量 | 276.21 |
| SMILES Code | CC(C)C(NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1)=O |
| MDL No. | MFCD00072009 |
| 别名 | SCH 13521; Niftolide; Testotard. FLUT.; Tecnoflut; Tafenil; Prostogenat; Prostica; Prostadirex; Prostacur; Profamid; Oncosal; Grisetin; Fugerel; Flutaplex; Flutan; Flutamin; Flutamex; FlutaGry; Flutacan; Flutabene; Flulem; Fluken; Flucinome; Eulexine; Euflex; Drogenil; Chimax; Apimid; Eulexin; Niftolid; Flugerel; Flucinom; NSC 251876; NSC 147834 |
| 运输 | 蓝冰 |
| InChI Key | MKXKFYHWDHIYRV-UHFFFAOYSA-N |
| Pubchem ID | 3397 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(380.15 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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