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Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells. Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.
In vivo, Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model.
Molecular Weight | 470.6 |
Formula | C30H34N2O3 |
CAS Number | 198481-32-2 |
Form | Solid |
Solubility (25°C) | DMSO 95 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Parth M. Raina, et al. Bazedoxifene
[4] No authors listed. Aust Prescr. Conjugated oestrogens/bazedoxifene
[5] No authors listed. Drug Ther Bull. Bazedoxifene for HRT?
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