63619-84-1
Chemical Structure
Trioxifene
Synonym(s): LY133314 free base
- CAS. Nr.: 63619-84-1
- Formula:C30H31NO3
- Molecular Weight:453.58
IUPAC Name: (2-(4-methoxyphenyl)-3,4-dihydronaphthalen-1-yl)(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)methanone
InChIKey: IHGLINDYFMDHJG-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(OCCN2CCCC2)C=C1)C=3C4=CC=CC=C4CCC3C=5C=CC(OC)=CC5
Biological Activity: Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma[1][2].
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Trioxifene | Trioxifene (LY133314 free base) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma. | |||||||||||||||||||||
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- [1]. Lee RW, et al. Trioxifene mesylate in the treatment of advanced breast cancer. Cancer. 1986;57(1):40-43. [Content Brief]
- [2]. Neubauer BL, et al. The selective estrogen receptor modulator trioxifene (LY133314) inhibits metastasis and extends survival in the PAIII rat prostatic carcinoma model. Cancer Res. 2003;63(18):6056-6062. [Content Brief]
Keywords
