货号:A561132
同义名:
宜利治
/ Megestryl Acetate; BDH1298
Megestrol acetate是一种合成孕激素,具有口服活性,可作为食欲刺激素,用于恶病质研究,并通过下调雄激素受体活性影响 HIV 和自噬相关疾病。


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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。 | |||||||||||||||||||
| 描述 | Megestrol acetate was one of the first progestational agents to be evaluated for use in the hormonal therapy of advanced breast cancer. As single-agent therapy, the average overall response rate to megestrol acetate therapy is 30%[3]. Megestrol acetate doses equal to or lower than 240 mg/day lead to slight weight gain in patients with cancer-associated cachexia[4]. The mechanism of action of megestrol is believed to involve stimulation of appetite by both direct and indirect pathways and antagonism of the metabolic effects of the principal catabolic cytokines[5]. The risk of megestrol-induced Cushing syndrome, especially with high doses of the medication, should be considered as a possible adverse effect in patents with renal insufficiency[6]. |
| Concentration | Treated Time | Description | References | |
| ECC-1 cells | 75 μM | 24 h | To study the effect of combining megestrol acetate with pterostilbene on endometrial cancer cell growth, the results showed that the combination significantly enhanced apoptosis and cell cycle inhibition. | Sci Rep. 2017 Oct 6;7(1):12754. |
| HEC-1A cells | 75 μM | 24 h | To study the effect of combining megestrol acetate with pterostilbene on endometrial cancer cell growth, the results showed that the combination significantly enhanced apoptosis and cell cycle inhibition. | Sci Rep. 2017 Oct 6;7(1):12754. |
| Endometrial cancer patient-derived organoids | 1 µM | 2 weeks | To evaluate the inhibitory effect of Megestrol on the growth of endometrial cancer organoids, results showed that Megestrol did not significantly inhibit organoid growth. | Int J Gynecol Cancer. 2017 Oct;27(8):1701-1707. |
| Administration | Dosage | Frequency | Description | References | ||
| Nude mice | HEC-1A xenograft model | Oral gavage | 10 mg/kg | Daily for 5 weeks | To study the effect of combining megestrol acetate with pterostilbene on tumor growth in an endometrial cancer xenograft model, the results showed that the combination significantly inhibited tumor growth. | Sci Rep. 2017 Oct 6;7(1):12754. |
| Nude mice | Ovarian cancer model | Subcutaneous injection | 250 µg | Daily, for 28 days | To study the effect of Megestrol on ovarian cancer growth, results showed that the combination of Megestrol with 17β-estradiol restored tumor burden to near control levels. | Clin Cancer Res. 2009 May 1;15(9):2971-8 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.60mL 0.52mL 0.26mL |
13.00mL 2.60mL 1.30mL |
26.01mL 5.20mL 2.60mL |
|
| CAS号 | 595-33-5 |
| 分子式 | C24H32O4 |
| 分子量 | 384.51 |
| SMILES Code | CC(O[C@]1(C(C)=O)CC[C@@]2([H])[C@]3([H])C=C(C)C4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O |
| MDL No. | MFCD00056470 |
| 别名 | 宜利治 ;Megestryl Acetate; BDH1298; Niagestin.; Megestil; Pallace. Maygace; Ovaban; Megace; NSC 71423; SC10363 |
| 运输 | 蓝冰 |
| 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: 18 mg/mL(46.81 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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