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他莫昔芬

他莫昔芬

品 牌 Sigma
C A S 号 10540-29-1
别 名 (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
货 号 T5648
规 格 1g
价 格(元) 2390.00
咨询优惠价
货号 规格 价格
T5648 1g 2390.00

产品说明

Frequently Asked Questions
Frequently Asked Questions are available for this Product.
General description
Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen is a prodrug that is metabolized to active metabolites 4-hydroxytamoxifen (4-OHT) and endoxifen by cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the gene repressor activity of tamoxifen against ERBB2 is dependent upon PAX2. Blocks estradiol-stimulated VEGF production in breast tumor cells.
包装
1, 5 g in glass bottle
Preparation Note
Tamoxifen is soluble in chloroform at 50 mg/ml and yields a clear, colorless to faint yellow solution. It is also soluble in methanol, ethanol, 2-propanol and propylene glycol. Stock solutions of tamoxifen can also be prepared in DMSO at 10 mM. However, it is practically insoluble in water (solubility is <0.01%, 20° C). Solutions are sensitive to UV light, and DMSO solutions are stable when stored at -20° C in the dark.
Application
Tamoxifen has been used to facilitate the recombination of ect2flox allele in mouse organs91. It has also been used to study its effect on lipopolysaccharide (LPS)-induced microglial activation92.
Biochem/physiol Actions
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。
Features and Benefits
This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.


性质:


Related Categories Antibiotics A to Z, Antibiotics T-Z, Antibiotics by Application, Antineoplastic and Immunosuppressive Antibiotics, Application Index,
InChI Key NKANXQFJJICGDU-QPLCGJKRSA-N
assay ≥99%
mp 97-98 °C(lit.)
solubility H2O: insoluble <0.1% at 20 °C
chloroform: soluble50 mg/mL, clear, colorless to faintly yellow
2-propanol: soluble
DMSO: soluble
ethanol: soluble
methanol: soluble
propylene glycol: soluble
originator AstraZeneca
storage temp. 2-8°C
Gene Information human ... CYP1A2(1544), EBP(10682), ESR1(2099), ESR2(2100), ESRRA(2101)
rat ... Ar(24208), Esr1(24890)
pKa (25 °C) 8.1
bp 219-220 °C/10 mmHg(lit.)
mp 167-172 °C(lit.)
solubility water: soluble (678 g/l at 20 °C)
absorption A40%/290 nm ≤0.05
Featured Industry Diagnostic Assay Manufacturing 10540-29-1