Gestodene-d6 is intended for use as an internal standard for the quantification of gestodene by GC- or LC-MS. Gestodene is a progestin.1 It selectively binds to the progesterone receptor over the estrogen receptor.2 Gestodene induces transcriptional activity mediated by the progesterone receptor, and, weakly, the androgen receptor in reporter assays.3 It increases the growth of MCF-7 cells when used at concentrations ranging from 0.1 to 1 µM.4 In contrast, gestodene (0.1 mg/kg) reduces tumor growth in an estrogen-dependent model of rat mammary tumors induced by DMBA . Formulations containing gestodene, in combination with ethynyl estradiol have been used as oral contraceptives.
1.Stanczyk, F.Z.All progestins are not created equalSteroids68(10-13)879-890(2003) 2.Pollow, K., Juchem, M., Grill, H.J., et al.Lack of binding of gestodene to estrogen receptor in human breast cancer tissueEur. J. Cancer26(5)608-610(1990) 3.Fuhrmann, U., Slater, E.P., and Fritzemeier, K.H.Characterization of the novel progestin gestodene by receptor binding studies and transactivation assaysContraception51(1)45-52(1995) 4.Kloosterboer, H.J., Schoonen, W.G., Deckers, G.H.J., et al.Effects of progestagens and Org OD14 in in vitro and in vivo tumor modelsJ. Steroid Biochem. Mol. Biol.49(4-6)311-318(1994)