The solution stability of this product in corn oil has not been determined. However, other sources state that solutions of tamoxifen in corn oil can be stored at 4°C for up to a week.
T5648
泰莫西芬
Tamoxifen
1 of 2 reviewers received a sample product or took part in a promotion
≥99% (TLC), powder, PKC inhibitor
同義詞:
反式他莫昔芬, (Z)-1-(对二甲基氨基乙氧基苯基)-1,2-二苯基-1-丁烯, (Z)-2-[4-(1,2-二苯基-1-丁烯)苯氧基]-N,N-二甲基乙胺
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About This Item
線性公式:
C6H5C(C2H5)=C(C6H5)C6H4OCH2CH2N(CH3)2
CAS號碼:
分子量：:
371.51
EC號碼:
MDL號碼:
分類程式碼代碼:
12161501
PubChem物質ID:
NACRES:
NA.54
暫時無法取得訂價和供貨情況
推薦產品
產品名稱
泰莫西芬, ≥99%
無菌
(Not packaged in a sterile environment)
化驗
≥99%
mp
97-98 °C (lit.)
溶解度
H2O: insoluble <0.1% at 20 °C
chloroform: soluble 50 mg/mL, clear, colorless to faintly yellow
2-propanol: soluble
DMSO: soluble
ethanol: soluble
methanol: soluble
propylene glycol: soluble
抗生素活性譜
neoplastics
作用方式
enzyme | inhibits
起源
AstraZeneca
儲存溫度
2-8°C
SMILES 字串
CC\C(c1ccccc1)=C(/c2ccccc2)c3ccc(OCCN(C)C)cc3
InChI
1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-
InChI 密鑰
NKANXQFJJICGDU-QPLCGJKRSA-N
基因資訊
human ... CYP1A2(1544) , EBP(10682) , ESR1(2099) , ESR2(2100) , ESRRA(2101)
rat ... Ar(24208) , Esr1(24890)
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一般說明
他莫昔芬(TC)是一种选择性雌激素受体调节剂(SERM)，用于治疗男性和女性乳腺癌。还可作为女性的癌症预防药物。[1]这种蛋白激酶C抑制剂和抗血管生成因子是一种前药，可通过细胞色素P450酶的同工型CYP2D6和CYP3A4代谢成活性代谢产物4-羟基他莫昔芬(4-OHT)和内昔芬。在乳腺癌中，他莫昔芬针对ERBB2的基因阻遏活性依赖于PAX2。在乳腺癌细胞中，他莫昔芬抑制雌二醇诱导的血管内皮生长因子受体(VEGF)生成。雌激素受体阳性肿瘤患者更有可能受益于他莫昔芬治疗。通过选择性结合机体不同部位的雌激素受体，他莫昔芬具有雌激素激动剂和拮抗剂作用。[1]
这种非类固醇三苯乙烯衍生物可抑制肿瘤生长，据报道是一种动物致癌物和致畸物。此外，他莫昔芬还保护骨骼免遭雌激素缺乏的骨丢失，降低血浆胆固醇，并参与大鼠的肝脏癌变过程。他莫昔芬的其他作用包括降低胰岛素样生长因子的血浆水平，诱导癌细胞包围的细胞分泌转化生长因子β，抑制膜脂质过氧化（可能通过降低膜流动性发挥作用）。
这种非类固醇三苯乙烯衍生物可抑制肿瘤生长，据报道是一种动物致癌物和致畸物。此外，他莫昔芬还保护骨骼免遭雌激素缺乏的骨丢失，降低血浆胆固醇，并参与大鼠的肝脏癌变过程。他莫昔芬的其他作用包括降低胰岛素样生长因子的血浆水平，诱导癌细胞包围的细胞分泌转化生长因子β，抑制膜脂质过氧化（可能通过降低膜流动性发挥作用）。
應用
他莫昔芬已用于：
- MTS (3-(4,5-二甲基噻唑-2-基)-5-(3-羧基甲氧基苯基)-2-(4-磺酸苯基)-2H-四唑) 试验和结晶紫染色试验，以评估细胞活力。[2] [3]
- 诱导Dicer条件性敲除小鼠中的Dicer消融，以研究Dicer缺乏对脂肪细胞分化和功能的作用。[4]
- 研究其对来源于T细胞急性成淋巴细胞性白血病（T-ALL）的耐糖皮质激素（GC）细胞系Jurkat的生物学作用。[5]
- 研究他莫昔芬治疗对小鼠中雌激素受体α（ERα）介导的下丘脑-POA的生理学作用。[6]
- 诱导Cre重组酶活性进行基因操控。[7]
- 促进ect2flox等位基因在小鼠器官中的重组。
- 研究其对脂多糖（LPS）诱导的小胶质细胞激活的影响。
生化／生理作用
蛋白激酶 C 抑制剂。诱发人类恶性神经胶质瘤细胞系的细胞凋亡。他莫昔芬及其代谢产物 4-羟基他莫昔芬是选择性雌激素反应调节剂 (SERM)，在乳腺中用作雌激素拮抗剂。阻止乳腺肿瘤细胞中雌二醇刺激的 VEGF 的产生。
特點和優勢
该化合物是ADME Tox研究的特色产品。点击此处以发现更多的ADME Tox特色产品。可访问sigma.com/discover-bsm了解更多关于用于其他研究领域生物活性小分子。
该化合物由AstraZeneca开发。如需浏览其他药物开发的化合物和批准的药物/候选药物清单，请单击此处。
準備報告
他莫昔芬可以50 mg/ml溶于氯仿并产生一种透明无色至淡黄色的溶液。它还可溶于甲醇、乙醇、2-丙醇和丙二醇。他莫昔芬的储备溶液可按10 mM制备于DMSO中。然而，它几乎不溶于水（溶解度是<0.01%, 20° C）。溶液对紫外光敏感，而DMSO溶液可避光稳定储存在 -20° C。
儲存和穩定性
Tamoxifen is relatively stable. The powder should be stable for at least two years when stored desiccated at 2-8C, protected from light.
其他說明
This product is not packaged in a sterile environment.
訊號詞
Danger
危險聲明
危險分類
Aquatic Acute 1 - Aquatic Chronic 1 - Carc. 1A - Repr. 1B
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
個人防護裝備
Eyeshields, Gloves, type P3 (EN 143) respirator cartridges
從最近期的版本中選擇一個：
分析證明 (COA)
Lot/Batch Number
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相關內容
探索蛋白質通路分析，包括化學庫篩選和使用小分子調節通路。
Chromatograms
application for HPLC, application for SPE-
Tamoxifen was dissolved in corn oil (20mg/ml concentration). Can this solution be stored long term and how? Thank you.
1 answer-
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Is this product pharmaceutical grade?
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This product is intended for research use only. At this time, a pharmaceutical-grade product option is not available.
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Hello, Thank you for your product. According to my protocol, I have to dissolve Tamoxifen in the corn oil at the final concentration of 40 mg/ml and feed my mice with that. However, it's insoluble. How can I resolve it? Thank you, Hossein
1 answer-
This product is soluble in chloroform (50 mg/mL, clear, colorless to faintly yellow), 2-propanol, DMSO (10 mM), ethanol, methanol and propylene glycol. Kindly review the information on the product datasheet available at this link: https://www.sigmaaldrich.com/deepweb/assets/sigmaaldrich/product/documents/389/852/t5648pis.pdf
Corn oil has also been used as a vehicle for tamoxifen as cited by Whitfield J, Littlewood T, Soucek L. Tamoxifen administration to mice. Cold Spring Harb Protoc. 2015 Mar 2;2015(3):269-71. doi: 10.1101/pdb.prot077966. PMID: 25734062; PMCID: PMC6773604. Kindly also review the details at this link: https://www.jax.org/research-and-faculty/resources/cre-repository/tamoxifen
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If I want to use 20mg of tamoxifen, could I only dissolve part of tamoxifen and then store the rest of the powder at refrigerator? Or do I have to dissolve all vial at once?
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Tamoxifen is relatively stable. Any required amount can be weighed up for use as needed and the bottle resealed. The powder should be stable for at least two years when stored desiccated at 2-8C, and protected from light.
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Is this product sterile?
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This product is not packaged in a sterile environment.
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What is the solubility of tamoxifen, Product No. T5648?
1 answer-
Tamoxifen is tested for solubility in chloroform at a concentration of 50mg/mL. This yields a colorless to faint yellow solution. Tamoxifen is practically insoluble in water. It has been reported to be soluble in methanol, ethanol, 2-propanol and propylene glycol. This product is also reported to be soluble in DMSO at 10mM concentration. Reference for DMSO solubility: Wong, K.R., et al., Am. J. Physiol. Heart Circ. Physiol., 277, H1403-H1409 (1999). Please also see the product information sheet (under Documents, above) for more information on the solubility of this product.
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What is the stability of tamoxifen (e.g., Product No. T5648) once in solution?
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Solutions of tamoxifen are sensitive to UV light. According to C.A. O'Brian et al., [Cancer Res. 45, 2462 (1985)], tamoxifen when dissolved in DMSO can be stored at -20°C in the dark. We generally recommend making the solution fresh right before each use.
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What is the Department of Transportation shipping information for this product?
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Transportation information can be found in Section 14 of the product's (M)SDS.To access the shipping information for this material, use the link on the product detail page for the product.
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How do I find the expiration date of the bottle of Product No T5648, Tamoxifen, in my possession?
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According to Sigma Quality Control Data, T5648 (tamoxifen) should be stable for at least two years if stored dessicated at 2-8°C in the dark. However, there is not an established expiration or retest date for Tamoxifen. This product is guaranteed for 1 year from shipment, if stored correctly and unopened.
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