A selective estrogen receptor modulator
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Bazedoxifene (acetate)

Item No. 15005

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol, acetate
CAS Number
198481-33-3
Synonyms
  • TSE 424
Molecular Formula
C30H34N2O3 • C2H4O2
Formula Weight
530.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:20): 0.04 mg/mlDMSO: 14 mg/mlEthanol: 5 mg/ml
λmax
227, 299 nm
SMILES
CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=C1C=C(O)C=C5.CC(O)=O
InChi Code
InChI=1S/C30H34N2O3.C2H4O2/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31;1-2(3)4/h6-15,20,33-34H,2-5,16-19,21H2,1H3;1H3,(H,3,4)
InChi Key
OMZAMQFQZMUNTP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    Bazedoxifene (acetate) is a third generation selective estrogen receptor modulator (SERM). It is an indole-based ER ligand that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM).1 Bazedoxifene (actetate) antagonizes 17β-estradiol-dependent MCF-7 and T47D breast cancer cell proliferation in vitro as well as hormone-independent growth of MCF-7:5C cells that are resistant to long-term estrogen deprivation (80% reduction with 10 nM).2 It has been shown to arrest cell cycling by downregulating cyclin D1 and ERα.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Komm, B.S., Kharode, Y.P., Bodine, P.V.N., et al. Bazedoxifene acetate: A selective estrogen receptor modulator with improved selectivity. Endocrinology 146(9), 3999-4008 (2005).

    2. Lewis-Wambi, J.S., Kim, H., Curpan, R., et al. The selective estrogen receptor modulator bazedoxifene inhibits hormone-independent breast cancer cell growth and down-regulates estrogen receptor α and cyclin D1. Mol. Pharmacol. 80(4), 610-620 (2011).