Molecular Formula | C19H26O3 |
Molar Mass | 302.41 |
Density | 1.178±0.06 g/cm3(Predicted) |
Melting Point | 188-190°C |
Boling Point | 464.4±45.0 °C(Predicted) |
Flash Point | 234.7°C |
Solubility | Soluble in DMSO (10 mg/mL), ethanol (10 mg/mL), chloroform, ethanol (1 mg/ml), and 1:1D |
Vapor Presure | 2E-09mmHg at 25°C |
Appearance | crystalline |
Color | light yellow |
Maximum wavelength(λmax) | ['286nm(EtOH)(lit.)'] |
pKa | 10.29±0.60(Predicted) |
Storage Condition | Inert atmosphere,Room Temperature |
Refractive Index | 1.586 |
MDL | MFCD00010489 |
Use | A disruptor of microtubule function and HIF-1 inhibitor |
In vitro study | 2-Methoxyestradiol acts on breast cancer cell line MDA-MB-435 and ovarian cancer cell line SK-OV-3 and inhibits cell proliferation with IC50 of 1.38 μm and 1.79 μm, respectively. Moreover, 2-Methoxyestradiol acts on rat aortic smooth muscle A- 10 cells and also inhibits cell microtubule depolymerization, with an EC50 of 7.5 μm. 2-Methoxyestradiol inhibited MCF-7 and BM cell proliferation with IC50 of 52 μm and 8 μm, respectively. 2-Methoxyestradiol acts on MDA-MB-231 cells to inhibit transcriptional activation of HIF-1-regulated target genes without affecting transcription of HIF-1α itself. Recent studies have shown that 2-Methoxyestradiol(0.5 μm) blocks TGF-β3 to induce collagen (Col)I (αi), Col III (αi), plasminogen activator inhibitor (PAI) 1, expression of connective tissue growth factor (CTGF), and α-smooth muscle actin (α-SMA). Furthermore, 2-Methoxyestradiol attenuated tgf-β3-induced Smad2/3 phosphorylation and nuclear translocation, and inhibited tgf-β3-induced activation of the PI3K/Akt/mTOR pathway. |
In vivo study | 2-Methoxyestradiol acts on 9L rat glioma model (9L-V6R), significantly reduces HIF-1 activity and inhibits tumor growth. This effect is dose-dependent, and is treated at a dose of 60 mg/kg per day, there was a 4-fold reduction in tumors and a 23-fold reduction in the 600 mg/kg daily dose. |
Risk Codes | R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. R48 - Danger of serious damage to health by prolonged exposure R61 - May cause harm to the unborn child R60 - May impair fertility R46 - May cause heritable genetic damage R45 - May cause cancer R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S22 - Do not breathe dust. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S53 - Avoid exposure - obtain special instructions before use. S36 - Wear suitable protective clothing. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9/PG 3 |
WGK Germany | 3 |
RTECS | KG7537500 |
Reference Show more | 1. [IF=7.711] Zhen Zhang et al."Mitochondria-Accessing Ratiometric Fluorescent Probe for Imaging Endogenous Superoxide Anion in Live Cells and Daphnia magna."Acs Sensors. 2018;3(3):735–741 |