Exemestane

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Chemical Structure| 107868-30-4 同义名 : FCE 24304; EXE
CAS号 : 107868-30-4
货号 : A718724
分子式 : C20H24O2
纯度 : 97%
分子量 : 296.4
MDL号 : MFCD00866994
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 55 mg/mL(185.56 mM)，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
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

生物活性
靶点

  • Aromatase

    Aromatase (human), IC50:30 nM

    Aromatase (rat), IC50:40 nM
描述 Exemestane is an aromatase inhibitor of human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human MCF7 cells 10 to 15 μM Cytotoxicity assay 3-6 days Cytotoxicity against human placental microsome aromatase expressing human MCF7 cells assessed as reduction in cell viability at 10 to 15 uM after 3 to 6 days by MTT assay in presence of estradiol 25277066
human MCF7a cells Cytotoxicity assay 10 days Cytotoxicity against human MCF7a cells expressing Tet-off-3betaHSD1-Arom assessed as inhibition of TST-stimulated cell proliferation measured after 10 days, EC50=5.6 nM 22951074
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00066703 Breast Cancer Phase 3 Active, not recruiting June 2020 -
NCT00066703 - Active, not recruiting - -
NCT03125746 Advanced Breast Cancer Phase 1 Recruiting February 28, 2020 China ... 展开 >> Cancer Hospital Chinese Academy of Medical Sciences Recruiting Beijing, China Contact: Binghe Xu, Doctor 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.37mL

0.67mL

0.34mL

16.87mL

3.37mL

1.69mL

33.74mL

6.75mL

3.37mL
参考文献

[1]Miki Y, Suzuki T, et al. Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone. 2007 Apr;40(4):876-87.

[2]Di Salle E, Briatico G, et al. Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol. 1994 Jun;49(4-6):289-94.