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Megestrol acetate/醋酸甲地孕酮 {[allProObj[0].p_purity_real_show]}

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。

Megestrol acetate/醋酸甲地孕酮 化学结构 CAS号:595-33-5
Megestrol acetate/醋酸甲地孕酮 化学结构
CAS号:595-33-5
Megestrol acetate/醋酸甲地孕酮 3D分子结构
CAS号:595-33-5
Megestrol acetate/醋酸甲地孕酮 化学结构 CAS号:595-33-5
Megestrol acetate/醋酸甲地孕酮 3D分子结构 CAS号:595-33-5
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Megestrol acetate/醋酸甲地孕酮 纯度/质量文件 产品仅供科研

货号:A561132 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Megestrol acetate/醋酸甲地孕酮 生物活性

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].

Megestrol acetate/醋酸甲地孕酮 细胞实验

Cell Line
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.

Megestrol acetate/醋酸甲地孕酮 动物实验

Species
Animal Model
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

Megestrol acetate/醋酸甲地孕酮 参考文献

[1]Sung JH, An HS, et al. Megestrol Acetate Increases the Proliferation, Migration, and Adipogenic Differentiation of Adipose-Derived Stem Cells via Glucocorticoid Receptor. Stem Cells Transl Med. 2015 Jul;4(7):789-99.

[2]Kelicen Ugur P, Lule S, et al. Megestrol acetate inhibits the expression of cytoplasmic aromatase through nuclear C/EBPβ in reperfusion injury-induced ischemic rat hippocampus. Eur J Pharmacol. 2011 Mar 11;654(3):217-25.

[3]Sedlacek SM. An overview of megestrol acetate for the treatment of advanced breast cancer. Semin Oncol. 1988 Apr;15(2 Suppl 1):3-13.

[4]Ruiz-García V, Juan O, Pérez Hoyos S, Peiró R, Ramón N, Rosero MA, García MA. Acetato de megestrol: una revisión sistemática de su utilidad clínica para la ganancia de peso en los enfermos con neoplasia y caquexia [Megestrol acetate: a systematic review usefulness about the weight gain in neoplastic patients with cachexia]. Med Clin (Barc). 2002 Jul 6;119(5):166-70. Spanish

[5]Femia RA, Goyette RE. The science of megestrol acetate delivery: potential to improve outcomes in cachexia. BioDrugs. 2005;19(3):179-87

[6]Caparrós GC, Zambrana JL, Delgado-Fernandez M, Díez F. Megestrol-induced Cushing syndrome. Ann Pharmacother. 2001 Oct;35(10):1208-10

Megestrol acetate/醋酸甲地孕酮 实验方案

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

Megestrol acetate/醋酸甲地孕酮 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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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