Tesmilifene is a novel agent that augments cytotoxicity of various chemotherapeutic agents both in vitro and in vivo. It binds selectively to the high-affinity microsomal antiestrogen binding site (Ki=50nm) but has no affinity for estrogen receptors. Inhibits concanavalin-A-induced histamine release in mast cells and acts as a novel antagonist of intracellular histamine.
Product Details
| Alternative Name: | DPPE, N,N-Diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine . HCl |
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| Formula: | C19H25NO . HCl |
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| MW: | 283.4 . 36.5 |
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| CAS: | 92981-78-7 |
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| MI: | 14: 9178 |
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| Purity: | ≥99% (TLC) |
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| Appearance: | Off-white solid. |
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| MeltingPoint: | 150-152°C |
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| Solubility: | Soluble in water (4mg/ml) or DMSO (3mg/ml). |
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| Shipping: | Ambient |
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| Long Term Storage: | Ambient |
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| Use/Stability: | Stable for at least 1 year after receipt when stored at -20°C.Stock solutions are stable for up to 3 months at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Enhancement of cytotoxicity of natural product drugs against multidrug resistant variant cell lines of human head and neck squamous cell carcinoma and breast carcinoma by tesmilifene.: P. J. Ferguson, et al.; Cancer Lett.
274, 279 (2009),
Abstract;
Phase III study of N,N-diethyl-2-[4-(phenylmethyl) phenoxy]ethanamine (BMS-217380-01) combined with doxorubicin versus doxorubicin alone in metastatic/recurrent breast cancer: National Cancer Institute of Canada Clinical Trials Group St: L. Reyno, et al.; J. Clin. Oncol.
22, 269 (2004),
Abstract;
Synergy between tamoxifen and cisplatin in human melanoma cells is dependent on the presence of antiestrogen-binding sites.: J.A. Jones, et al.; Cancer Res.
57, 2657 (1997),
Abstract;
Influence of DPPE on histamine release from isolated rat mast cells.: N. Grosman; Agents Actions
41, 1 (1994),
Abstract;
Histamine is an intracellular messenger mediating platelet aggregation.: S.P: Saxena, et al.; Science
243, 1596 (1989),
Abstract;
