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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white
溶解性
H2O: 16 mg/mL
储存温度
2-8°C
SMILES字符串
Cl.CCN(CC)CCOc1ccc(Cc2ccccc2)cc1
InChI
1S/C19H25NO.ClH/c1-3-20(4-2)14-15-21-19-12-10-18(11-13-19)16-17-8-6-5-7-9-17;/h5-13H,3-4,14-16H2,1-2H3;1H
InChI key
TXLHNFOLHRXMAU-UHFFFAOYSA-N
生化/生理作用
DPPE is a potent, selective ligand of the microsomal anti-estrogen binding site.
DPPE is a potent, selective ligand of the microsomal anti-estrogen binding site. DPPE is a tamoxifen derivataive that binds with high affinity to the anti-estrogen binding site, but unlike tamoxifen, does not bind to the estrogen receptor. DPPE sensitizes MDR tumor cells to chemotherapy and also inhibits histamine binding at the intracellular histamine site.
特点和优势
This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
储存分类代码
11 - Combustible Solids
WGK
nwg
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Proceedings of the Western Pharmacology Society, 50, 61-63 (2008-07-09)
N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine (DPPE, tesmilifene), a potent chemopotentiating drug currently in Phase III clinical trials of metastatic breast cancer, increases cytotoxicity of anthracyclines and taxanes in a variety of multi-drug resistance expressing (MDR+) tumor cell lines in vitro; inhibits binding of histamine
Breast cancer research and treatment, 49(1), 61-68 (1998-08-07)
N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine.HCl (DPPE) is a diphenylmethane analog of tamoxifen that antagonizes the intracellular binding of histamine to growth-regulatory sites, a proportion of which represents P450 enzymes, in microsomes and nuclei. We previously reported increased response rates and decreased myelotoxicity in
General pharmacology, 30(2), 195-200 (1998-03-21)
1. We have investigated the ability of several compounds to diminish both infarct area and volume induced by middle cerebral artery occlusion in the mouse. 2. Lifarizine, ipsapirone and N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE) all reduced both infarct area and volume. Ifenprodil
Melanoma research, 12(3), 231-240 (2002-07-26)
Histamine is produced by many cells expressing histidine decarboxylase (HDC), the enzyme responsible for the synthesis of histamine. Since melanoma cells and tissue contain relatively large amounts of histamine, the functional significance of histamine was examined using specific antihistamines in
European journal of cancer (Oxford, England : 1990), 33(1), 122-128 (1997-01-01)
This study was designed to the elucidate sensitising effects of the intracellular histamine antagonist, N,N-diethyl-2[4-(phenylmethyl)phenoxy] ethanamine HCl (DPPE) on the antitumour activity of cis-diamminedichloroplatinum (II) (CDDP) using human ovarian cancer cell lines with different sensitivities to CDDP (KF, sensitive) KFra
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