2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Trioxifene mesylate

Trioxifene mesylate (LY133314) 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 mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma.

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Trioxifene mesylate

Trioxifene mesylate 構造式

CAS 番号 : 68307-81-3

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Trioxifene mesylate 関連抗体

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Estrogen Receptor/ERR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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製品説明

Trioxifene mesylate (LY133314) 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 mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma[1][2].

IC50 & Target

hERα

203.49 nM (IC50)

hERα

20.84 nM (Ki)

hERβ

1506.04 nM (IC50)

hERβ

144.85 nM (Ki)

体外実験

Trioxifene (0.3-10000 nM; 4 h) mesylate binds to purified human recombinant ERα with human ERα IC50 of 203.49 nM and Ki of 20.84 nM[2].
Trioxifene (0.1-10.0 μM; 24 h) mesylate weakly antagonizes ERα-mediated gene expression in PAIII rat prostatic adenocarcinoma cells but does not alter ERβ-mediated gene expression in these cells[2].
Trioxifene (7 days) mesylate inhibits the proliferation of PAIII rat prostatic adenocarcinoma cells in vitro with an IC50 of 4.6 μM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trioxifene mesylate 関連抗体
体内実験

Trioxifene mesylate exhibits significant antitumor activity in DMBA (HY-W011845)-induced rat mammary carcinoma[1].
Trioxifene (2.0-40.0 mg/kg; s.c.; daily; 28 days or continuously until death) mesylate significantly inhibits PAIII prostatic adenocarcinoma metastasis to lymph nodes and lungs, reduces male accessory sex organ weight, and extends mean survival to 64.44 days with continuous 40.0 mg/kg-day administration in male LW rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LW (male, 110-125 g, injected s.c. with 1×106 PAIII prostatic adenocarcinoma cells in the dorsal tail)[2]
Dosage: 2.0 mg/kg; 4.0 mg/kg; 20.0 mg/kg; 40.0 mg/kg
Administration: s.c.; daily; 28 days or continuously until death
Result: Produced significant (P < 0.05) inhibition of PAIII metastasis, with maximum 86% reduction in gluteal lymph node weight, 88% reduction in iliac lymph node weight, and 98% reduction in pulmonary foci count at 40.0 mg/kg-day for 28 days.
Did not reduce primary tail tumor weight at any dose.
Induced dose-related, significant (P < 0.05) regression of male accessory sex organs, with maximum 76% reduction in normalized ventral prostate weight and 64% reduction in normalized seminal vesicle weight at 40.0 mg/kg-day for 28 days.
Caused significant (P < 0.05) dose-related decreases in final-to-initial body weight ratios, with a maximum 31% reduction at 40.0 mg/kg-day for 28 days.
Increased normalized testicular weights significantly (P < 0.05), though absolute testicular weights did not differ from controls.
Extended mean survival to 50.11 days in rats treated with 40.0 mg/kg-day for 28 days followed by vehicle, significantly longer than vehicle controls (41.78 days).
Extended mean survival to 64.44 days in rats treated continuously with 40.0 mg/kg-day until death, significantly longer than both vehicle controls and the 28-day treatment group.
分子量

549.68

分子式

C31H35NO6S
CAS 番号
SMILES

O=C(C1=C(C2=CC=C(OC)C=C2)CCC3=C1C=CC=C3)C4=CC=C(OCCN5CCCC5)C=C4.CS(=O)(O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献
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Trioxifene mesylate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trioxifene68307-81-3LY133314LY 133314LY-133314Estrogen Receptor/ERRPAIII rat prostatic adenocarcinoma cellsmale accessory sex organsmale LW ratsDMBA-induced rat mammary carcinomaimmature Holtzman ratsimmature Standard Cox miceERαestrogen receptor modulatoradult ovariectomized CD-1 miceERβInhibitorinhibitorinhibit

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