产品说明书

2-Methoxyestradiol

Print
Chemical Structure| 362-07-2 同义名 : 二甲氧基雌二醇 ;2-ME2;NSC-659853;US brand name: Panzem. Abbreviation: 2-ME2.;2-Methoxy Estradiol. 2-methoxyestradiol;2-ME;Panzem;2-Hydroxyestradiol 2-methyl ether;2-MeOE2
CAS号 : 362-07-2
货号 : A200225
分子式 : C19H26O3
纯度 : 98%
分子量 : 302.408
MDL号 : -
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(826.7 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
动物实验配方：

2%DMSO+30%PEG300+5%Tween 80+water 5 mg/mL

生物活性
靶点

  • HIF
描述 The response of mammalian cells to hypoxia is mediated by a family of transcription factors known as HIF (hypoxia-inducible factors). The subunits of HIF, HIF-1α and HIF-2α are structurally similar and can be degraded rapidly under normoxia. 2-Methoxyestradiol can inhibit HIF-1α and HIF-2α expression, as well as depolymerize microtubules. Treatment with 2-Methoxyestradiol (5 - 100 μM) for 16h can reduce expression of HIF-1α dose-dependently in PC-3 and MDA-MB-231 cells, accompanied with the reduced activity of HIF-1 and the expression of its target protein, VEGF, and without effect on HIF-1α mRNA levels or rate of protein degradation. Treatment with 2-Methoxyestradiol (10 - 100 μM) overnight can depolymerize microtubules and impair nuclear accumulation of HIF-1α in PC-3 cells under hypoxia. Daily oral administration of 2-Methoxyestradiol, 150 mg/kg, for 33 days suppressed tumor growth and angiogenesis, as well as depolymerized microtubules in breast cancer orthotopic models. The inhibition of HIF-2α expression and microtubule-depolymerization by 2-Methoxyestradiol can also be observed in endothelial cells[1].
作用机制 2-Methoxyestradiol inhibits the expression, nuclear accumulation and transcriptional activity of HIF-1α[1]. However, the accurate mechanism of action is unknown now.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
DU145 Growth inhibitory assay GI50=1.22 μM 17696419
DU-145 ~100 μM cytotoxicity assay GI50=1.8 μM 9240348
HCT-116 ~100 μM cytotoxicity assay GI50=0.47 μM 9240348
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.31mL

0.66mL

0.33mL

16.53mL

3.31mL

1.65mL

33.07mL

6.61mL

3.31mL
参考文献

[1]Mabjeesh NJ, Escuin D, et al. 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF. Cancer Cell. 2003 Apr;3(4):363-75.

[2]Sibonga JD, Lotinun S, et al. Dose-response effects of 2-methoxyestradiol on estrogen target tissues in the ovariectomized rat. Endocrinology. 2003 Mar;144(3):785-92.

[3]Kang SH, Cho HT, et al. Antitumor effect of 2-methoxyestradiol in a rat orthotopic brain tumor model. Cancer Res. 2006 Dec 15;66(24):11991-7.

[4]Evaluation of the PharmacokineticPharmacodynamic relationship, Metabolism and Plasma Protein Binding of the novel antitumor agent, 2-Methoxyestradiol (2ME2), following oral administration in patients with solid tumors.