2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa.
Sci Rep. 2016 Jul 1;6:28612.
Inhibition of hypoxia inducible factor-1α attenuates abdominal aortic aneurysm progression through the down-regulation of matrix metalloproteinases.
2-Methoxyestradiol purchased from AbMole
Cell Experiment | |
---|---|
Cell lines | MCF-7 and MDA-MB-231 cells |
Preparation method | Cell culture and cell treatment. MCF-7 estrogen receptor-positive (ER+ve) human breast cancer cells, MDA-MB-231 ER-negative (ER−ve) human breast cancer cells were obtained from the American Type Culture Collection (LGC Promochem, Teddington, UK). Cells were routinely cultured in RPMI-1640 medium supplemented with 10% (v/v) fetal calf serum, 1% L-glutamine (200 mM), 1% non-essential amino acids (100 ×) and 1% bicarbonate (7.5%) from Sigma and maintained in a humidified incubator under 5% CO2 atmosphere at 37°C. For experiments using hypoxic conditions, cells were incubated under 1% O2 and 5% CO2 atmosphere at 37°C. |
Concentrations | 0.5 μM |
Incubation time | 18 h |
Animal Experiment | |
---|---|
Animal models | mice bearing MCF-7 and MDA-MB-231 xenografts model |
Formulation | 10% tetrahydrofuran: 90% propylene glycol |
Dosages | 40 or 75 mg/kg |
Administration | orally daily for 28 days |
Molecular Weight | 302.41 |
Formula | C19H26O3 |
CAS Number | 362-07-2 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Lakhani NJ, et al. Pharmacotherapy. 2-Methoxyestradiol, a promising anticancer agent.
Related HIF Products |
---|
Arylsulfonamide 64B
Arylsulfonamide 64B is a HIF-1α/2α inhibitor that can be used in studies related to uveal melanoma. |
PT-2567
PT-2567 is a HIF-2α inhibitor that can be used in studies related to pulmonary arterial hypertension. |
PMG-301
PMG-301 is a HIF-2α inhibitor that can be used in studies related to kidney tumors. |
K1299
K1299 is a HIF-2α inhibitor that can be used in studies related to renal cell carcinoma. |
DFF332
DFF332 is a HIF-2α inhibitor that can be used in studies related to renal cell carcinoma. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.