Gestodene-d6 (Synonyms: SHB 331-d6; WL 70-d6)

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)