CAS: 97818-83-2

Applications (Z)-Chlorolefin-13C6 is an intermediate in the synthesis of Tamoxifen-13C6 (T006002), which is a labeled Tamoxifen; 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.Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen (H954725) are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-sti References Sutherland, R., et al.: Nature, 267, 434 (1977); Lerner, L., et al.: Cancer Res., 50, 4177 (1990); Love, R., et al.: J. Clin. Oncol., 20 2559 (2002);

Applications Intermediate in the prepration of Tamoxifen derivatives. References Stanciuc, O., et al.: J. Pharm. Sci., 82, 927 (1993), Laios, I., et al.: J. Steroid Biochem. Mol. Biol., 87, 207 (2004),

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Applications Intermediate in the prepration of Tamoxifen derivatives.