Toggle Nav


In stock
Catalog No.
anti-cancer agent acting as an angiogenesis inhibitor via the HIF-1a pathway
Grouped product items
SizePriceStock Qty
In stock
In stock
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

2-Hydroxyestradiol is an angiogenesis inhibitor via the HIF-1a pathway.

HIF-1a, a basic helix-loop-helix PAS domain containing protein, is reported as the master transcriptional regulator of cellular and developmental response to hypoxia.

In vitro: In vitro evidences suggested that most of the cellular effects of 2-hydroxyestradiol were mediated by 2-methoxyestradiol, a metabolite of 2-hydroxyestradiol as an anti-cancer agent acting as an angiogenesis inhibitor via the HIF-1a pathway. Inhibition of catechol-O-methyltransferase (COMT), the enzyme methylating 2-hydroxyestradiol to 2-methoxyestradiol, blocked the ability of 2-hydroxyestradiol to inhibit growth of vascular smooth muscle cells, cardiac fibroblasts, as well as renal mesangial cells. Moreover, 2-hydroxyestradiol could inhibit vascular smooth muscle cell growth in cells obtained from wild-type mice but not in cells cultured from COMT knockout mice. In contrast to 2OHE, treatment of vascular smooth muscle cells with 2-methoxyestradiol inhibited serum-induced growth of cells from both wild-type and COMTknockout mice [1].

In vivo: Animal study showed that after administration of 2-hydroxyestradiol, plasma levels of 2-hydroxyestradiol declined extremely rapidly. Concomitant with the disappearance of 2-hydroxyestradiol, 2-methoxyestradiol occurred and then declined. After administration of 2-methoxyestradiol, plasma levels of 2MEOE declined with a plasma CL of 50 ml min(-1) kg(-1). We could not detect 2-hydroxyestradiol in plasma from rats receiving 2-methoxyestradiol. Thus, the authors conclude that the conversion of 2-hydroxyestradiol to 2-methoxyestradiol was so efficient, and the administration of 2-hydroxyestradiol is bioequivalent to administration of 2-methoxyestradiol itself [1].

Clinical trial: So far, no clinical study has been conducted.

[1] Zacharia, L. C.,Piché, C.A.,Fielding, R.M., et al. 2-hydroxyestradiol is a prodrug of 2-methoxyestradiol. Journal of Pharmacology and Experimental Therapeutics 309(3), 1093-1097 (2004).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
Cas No.362-05-0
Synonyms2-HE2,NSC 61711
Solubility≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Nameestra-1,3,5(10)-triene-2,3,17β-triol
SDFDownload SDF
Canonical SMILESOC1=C(O)C=C(CC[[email protected]]2([H])[[email protected]]3([H])CC[[email protected]@]4(C)[[email protected]@]2([H])CC[[email protected]@H]4O)C3=C1
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure