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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- CAS 番号: 63619-84-1
- 分子式: C30H31NO3
- 分子量:453.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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hERα 203.49 nM (IC50) |
hERα 20.84 nM (Ki) |
hERβ 1506.04 nM (IC50) |
hERβ 144.85 nM (Ki) |
Trioxifene (0.3-10000 nM; 4 h) 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) 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) 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 (2.0-40.0 mg/kg; s.c.; daily; 28 days or continuously until death) 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.
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Animal Model:LW (male, 110-125 g, injected s.c. with 1×106 PAIII prostatic adenocarcinoma cells in the dorsal tail)[2]
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Dosage:2.0 mg/kg; 4.0 mg/kg; 20.0 mg/kg; 40.0 mg/kg
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Administration:s.c.; daily; 28 days or continuously until death
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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.
化学情報
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CAS 番号 63619-84-1
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分子量 453.58
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分子式 C30H31NO3
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SMILES
O=C(C1=CC=C(OCCN2CCCC2)C=C1)C=3C4=CC=CC=C4CCC3C=5C=CC(OC)=CC5
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別名
LY133314 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
- Trioxifene
- 63619-84-1
- LY133314
- LY 133314
- LY-133314
- Estrogen Receptor/ERR
- PAIII rat prostatic adenocarcinoma cells
- male accessory sex organs
- male LW rats
- DMBA-induced rat mammary carcinoma
- immature Holtzman rats
- immature Standard Cox mice
- ERα
- estrogen receptor modulator
- adult ovariectomized CD-1 mice
- ERβ
- Inhibitor
- inhibitor
- inhibit