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A new triphenylethylene derivative, TAT-59; hormone receptors; insulin-like growth factor 1; and growth suppression of hormone-dependent MCF-7 tumors in athymic mice.

Abstract
TAT-59 ((E)-4-[1-[4-[2-(dimethylamino)ethoxy]-phenyl]-2-(4- isopropyl)phenyl-1-butenyl]-phenyl-monophosphate) treatment was performed on hormone-dependent MCF-7 tumors in athymic mice. TAT-59 given at 1, 5, and 20 mg/kg inhibited the estrogen-stimulated growth of MCF-7 tumors in athymic mice in a dose-dependent fashion. The most clear decrease in tumor growth was shown in the TAT-59 alone group, although it was not dramatic. Average serum concentrations of DP-TAT-59((Z)-[1-[4-[2-(dimethylamino)- ethoxy]phenyl]-2-(4-isopropyl)phenyl-1-butenyl]-4-hydroxybenzene) and DM-DP-TAT-59(desmethyl-DP-TAT-59), metabolites of TAT-59, increased in a dose-dependent manner. Much higher levels of DP-TAT-59 and DM-DP-TAT-59 were shown in tumors (target tissues of estrogen) as compared with muscles (nontarget tissues of estrogen) or serum. A serum concentration of DP-TAT-59 or DM-DP-TAT-59 corresponding to the physiologic levels of serum estradiol in premenopausal women was sufficient to inhibit the estrogen-stimulated growth of MCF-7 tumors in mice. TAT-59 induced a dose-dependent increase in estrogen receptor levels in the MCF-7 tumors. In contrast, it prevented the estradiol (E2)-induced increase in progesterone receptor levels in a dose-dependent manner. Insulin-like growth factor 1 levels measured in the MCF-7 tumors significantly decreased in the TAT-59 alone group and in the no treatment group as compared with the E2 alone group. These results show the pronounced antiestrogenic action of TAT-59 on hormone-dependent MCF-7 tumors in athymic mice.
AuthorsY Iino, Y Takai, T Ando, S Ohwada, T Yokoe, N Sugamata, H Takei, J Horiguchi, K Iijima, Y Morishita
JournalCancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 34 Issue 5 Pg. 372-6 ( 1994) ISSN: 0344-5704 [Print] Germany
PMID8070003 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Estrogen Antagonists
  • Receptors, Estrogen
  • Tamoxifen
  • TAT 59
  • 2-(4-(1-(4-hydroxyphenyl)-2-(4-isopropylphenyl)-1-butenyl)phenoxy)-N,N-dimethylethylamine
  • Estradiol
  • Insulin-Like Growth Factor I
Topics
  • Animals
  • Antineoplastic Agents (blood, metabolism, therapeutic use)
  • Chromatography, High Pressure Liquid
  • Dose-Response Relationship, Drug
  • Estradiol (blood)
  • Estrogen Antagonists (blood, metabolism, therapeutic use)
  • Female
  • Insulin-Like Growth Factor I (drug effects)
  • Mammary Neoplasms, Experimental (drug therapy, metabolism)
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Muscles (metabolism)
  • Neoplasms, Hormone-Dependent (drug therapy, metabolism)
  • Random Allocation
  • Receptors, Estrogen (drug effects)
  • Tamoxifen (analogs & derivatives, blood, metabolism, therapeutic use)
  • Uterus (drug effects)

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