Endoxifen hydrochloride - CAS 1197194-41-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C25H28ClNO2
Molecular Weight:
409.95
COA:
Inquire
Targets:
Estrogen Receptor/ERR
Description:
Endoxifen hydrochloride is a metabolite of Tamoxifen and a selective estrogen receptor modulator (SERM) that inhibits the growth of estrogen-stimulated BT474 cells (IC50 = 54 nM). Endoxifen is used for the treatment of estrogen receptor (ER) positive breast cancer.
Brife Description:
SERM, breast cancer
Purity:
99%
Related CAS:
112093-28-4 (free base)
Synonyms:
4-[1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-Phenol hydrochloride (1:1)
MSDS:
Inquire
Application:
anticancer drug
InChIKey:
RPFIMPDXTABYCN-BJFQDICYSA-N
InChI:
InChI=1S/C25H27NO2.ClH/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;/h4-16,26-27H,3,17-18H2,1-2H3;1H/b25-24-;
Canonical SMILES:
CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl
1.The effects of a novel hormonal breast cancer therapy, endoxifen, on the mouse skeleton.
Gingery A;Subramaniam M;Pitel KS;Reese JM;Cicek M;Lindenmaier LB;Ingle JN;Goetz MP;Turner RT;Iwaniec UT;Spelsberg TC;Hawse JR PLoS One. 2014 May 22;9(5):e98219. doi: 10.1371/journal.pone.0098219. eCollection 2014.
Endoxifen has recently been identified as the predominant active metabolite of tamoxifen and is currently being developed as a novel hormonal therapy for the treatment of endocrine sensitive breast cancer. Based on past studies in breast cancer cells and model systems, endoxifen classically functions as an anti-estrogenic compound. Since estrogen and estrogen receptors play critical roles in mediating bone homeostasis, and endoxifen is currently being implemented as a novel breast cancer therapy, we sought to comprehensively characterize the in vivo effects of endoxifen on the mouse skeleton. Two month old ovariectomized C57BL/6 mice were treated with vehicle or 50 mg/kg/day endoxifen hydrochloride via oral gavage for 45 days. Animals were analyzed by dual-energy x-ray absorptiometry, peripheral quantitative computed tomography, micro-computed tomography and histomorphometry. Serum from control and endoxifen treated mice was evaluated for bone resorption and bone formation markers. Gene expression changes were monitored in osteoblasts, osteoclasts and the cortical shells of long bones from endoxifen treated mice and in a human fetal osteoblast cell line. Endoxifen treatment led to significantly higher bone mineral density and bone mineral content throughout the skeleton relative to control animals.
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CAS 1197194-41-4 Endoxifen hydrochloride

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