2-Methoxyestradiol (2-MeOE2)

製品コードS1233 バッチS123307

印刷

化学情報

Chemical Structure Synonyms NSC 659853, 2-ME2 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H26O3
分子量 302.41 CAS No. 362-07-2
Solubility (25°C)* 体外 DMSO 60 mg/mL (198.4 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
10%DMSO 40%PEG300 5%TWEEN80 45%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 6.000mg/ml (19.84mM) Taking the 1 mL working solution as an example, add 100 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 2-Methoxyestradiol (2-MeOE2, NSC 659853, 2-ME2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. 2-Methoxyestradiol induces both autophagy and apoptosis in various carcinogenic cell lines.
in vitro

2-Methoxyestradiol (2-MeOE2) exhibits the inhibitory activity of cellular proliferation in a breast carcinoma cell line MDA-MB-435 and an ovarian carcinoma cell line SK-OV-3 with IC50 of 1.38 μM and 1.79 μM, respectively. Furthermore, it also inhibits cellular microtubule depolymerization in rat aortic smooth muscle A-10 cells with EC50 of 7.5 μM. [1] This compound inhibits proliferation of MCF-7 and BM cells with IC50 of 52 μM and 8 μM. [2] In MDA-MB-231 cells, it inhibits HIF-1-mediated transcriptional activation of target genes without affecting the transcription of HIF-1α itself. [3] A recent study shows that 2-Methoxyestradiol (0.5 μM), blocks TGF-β3-induced expression of collagen (Col) type I(αI), Col III(αI), plasminogen activator inhibitor (PAI) 1, connective tissue growth factor (CTGF), and α-smooth muscle actin (α-SMA). Moreover, it ameliorates TGF-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibits TGF-β3-induced activation of the PI3K/Akt/mTOR pathway. [4]
in vivo

In a 9L rat glioma (9L-V6R) rat model, 2-Methoxyestradiol (2-MeOE2) significantly decreases HIF-1 activity and inhibits the tumor growth in a dose-dependent manner by 4-fold reduction for 60 mg/kg/day, and 23-fold reduction for 600 mg/kg/day, respectively. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Microtubule depolymerizing activity
The effects of 2-Methoxyestradiol (2-MeOE2) on cellular microtubule depolymerization are determined by indirect immunofluorescence techniques in rat aortic smooth muscle A-10 cells. Microtubules are visualized using a β-tubulin antibody. Three viewers determine the percent microtubule loss for each treatment concentration. The data are averaged and plotted as percent microtubule loss versus drug concentration, and the EC50s for microtubule depolymerization are calculated from the log dose–response curves.
細胞アッセイ 細胞株 MDA-MB-435 and SK-OV-3
濃度 0-20 μM
反応時間 48 hours
実験の流れ

The sulforhodamine B (SRB) assay is used to evaluate the antiproliferative activity of 2-Methoxyestradiol (2-MeOE2) in the MDA-MB-435 and SK-OV-3 cell lines. Cells are plated into 96-well plates and allowed to grow and attach for 24 hours followed by addition of this compound or vehicle controls. The cells are incubated with drugs for 48 hours and then the cellular protein is fixed, stained, and concentration determined by absorbance at 560 nm. Log dose–response curves are constructed for each experiment and the IC50 for inhibition of proliferation determined.
動物実験 動物モデル 9L-V6R cells are injected into the brains of Fischer 344 rats
投薬量 ≤600 mg/kg
投与方法 Administered via i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/12441194/
  • https://pubmed.ncbi.nlm.nih.gov/12711011/
  • https://pubmed.ncbi.nlm.nih.gov/12726862/
  • https://pubmed.ncbi.nlm.nih.gov/22579131/
  • https://pubmed.ncbi.nlm.nih.gov/17178898/
  • https://pubmed.ncbi.nlm.nih.gov/21115915/
  • https://pubmed.ncbi.nlm.nih.gov/25218350/

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2015, 6(4): 2250-62]

Data from [Data independently produced by , , Nucleic Acids Res, 2015, 43(10): 5081-98 ]

Data from [Data independently produced by , , Mol Cell Endocrinol, 2018, doi:10.1016/j.mce.2018.05.002]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Histone methyltransferase ASH1L primes metastases and metabolic reprogramming of macrophages in the bone niche [ Nat Commun, 2025, 16(1):4681] PubMed: 40394007
Combined Graphene Oxide with 2-Methoxyestradiol for Effective Anticancer Therapy in-vitro Model [ Int J Nanomedicine, 2025, 20:933-950] PubMed: 39850060
EBV-associated epithelial cancers cells promote vasculogenic mimicry formation via a secretory cross-talk with the immune microenvironment [ Theranostics, 2024, 14(13):5123-5140] PubMed: 39267775
IL-33 Accelerates Chronic Atrophic Gastritis through AMPK-ULK1 Axis Mediated Autolysosomal Degradation of GKN1 [ Int J Biol Sci, 2024, 20(6):2323-2338] PubMed: 38617533
The ANGPTL4-HIF-1α loop: a critical regulator of renal interstitial fibrosis [ J Transl Med, 2024, 22(1):649] PubMed: 38992710
The role of HIF-1α/BNIP3/mitophagy in acrylonitrile-induced neuronal death in HT22 cells and mice: A potential neuroprotection target [ Chem Biol Interact, 2024, 406:111327] PubMed: 39615733
HIF-1 inhibition reverses opacity in a rat model of galactose-induced cataract [ PLoS One, 2024, 19(2):e0299145] PubMed: 38416732
MiR-122-5p regulates the mevalonate pathway by targeting p53 in non-small cell lung cancer [ Cell Death Dis, 2023, 14(4):234] PubMed: 37005437
Signaling metabolite succinylacetone activates HIF-1α and promotes angiogenesis in GSTZ1-deficient hepatocellular carcinoma [ JCI Insight, 2023, 8(23)e164968] PubMed: 37906252
Ginkgo biloba extract attenuates cisplatin-induced renal interstitial fibrosis by inhibiting the activation of renal fibroblasts through down-regulating the HIF-1α/STAT3/IL-6 pathway in renal tubular epithelial cells [ Phytomedicine, 2023, 115:154809] PubMed: 37087791

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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