24320-06-7
24320-06-7
Chemical Structure
ORG 2058
- CAS No.: 24320-06-7
- Formula:C22H32O3
- Molecular Weight:344.49
InChIKey: IJLXLZGJDSJGIQ-BILPMHSYSA-N
SMILES: C[C@@]12[C@](C[C@H]([C@@H]2C(CO)=O)CC)([H])[C@@]3([H])[C@]([C@]4([H])C(CC3)=CC(CC4)=O)([H])CC1
Biological Activity: ORG 2058 is a progesterone receptor agonist with a Kd of 1.25-1.68 nM. ORG 2058 exhibits nuclear uptake/retention, activates progesterone-specific receptor-chromatin binding, induces apoptosis, inhibits normal breast epithelial proliferation and bcl-2/bclxL expression, and induces hydroxysteroid dehydrogenase activity. ORG 2058 can be used in breast cancer research[1][2][3][4][5][6][7][8][9].
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ORG 2058 | ORG 2058 is a progesterone receptor agonist with a Kd of 1.25-1.68 nM. ORG 2058 exhibits nuclear uptake/retention, activates progesterone-specific receptor-chromatin binding, induces apoptosis, inhibits normal breast epithelial proliferation and bcl-2/bclxL expression, and induces hydroxysteroid dehydrogenase activity. ORG 2058 can be used in breast cancer research. | |||||||||||||||||||||
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References
- [1]. Weaker FJ, et al. Autoradiographic localization of3H-ORG 2058, a synthetic progestin, in the mammary glands of the baboon. Breast Cancer Research and Treatment. 1984 Jun;4(2):143-7. [Content Brief]
- [2]. Traish AM, et al. 7α-17α-Dimethyl-19-nortestosterone (mibolerone) induces conformational changes in progesterone receptors distinct from those induced by ORG 2058. Steroids. 1994 Jun 1;59(6):362-70. [Content Brief]
- [3]. Gompel A, et al. In vitro studies of tibolone in breast cells. Fertility and sterility. 2002 Aug;78(2):351-9. [Content Brief]
- [4]. Geier A, et al. Differences in the association of the progesterone receptor ligated by antiprogestin RU38486 or progestin ORG 2058 to chromatin components. Biochimica et biophysica acta. 1987 Oct 22;931(1):78-86.
- [5]. Bakos T, et al. Steroids 51. An improved synthesis of ORG 2058 and the synthesis of [3H]ORG 2058. Steroids. 1993 Mar;58(3):115-8. [Content Brief]
- [6]. Koga M, et al. Modulation of the growth-inhibitory effects of progestins and the antiestrogen hydroxyclomiphene on human breast cancer cells by epidermal growth factor and insulin. Cancer research. 1989 Jan 1;49(1):112-6. [Content Brief]
- [7]. Šauer P, et al. Two synthetic progestins and natural progesterone are responsible for most of the progestagenic activities in municipal wastewater treatment plant effluents in the Czech and Slovak republics. Water research. 2018 Jun 15;137:64-71. [Content Brief]
- [8]. Houtman CJ, et al. Characterisation of (anti-)progestogenic and (anti-)androgenic activities in surface and wastewater using high resolution effectdirected analysis. Environment international. 2021 Aug;153:106536. [Content Brief]
- [9]. Heubner A, et al. High-performance and ion-exchange chromatography and chromatofocusing of the human uterine progesterone receptor: its application to the identification of 21-[3H] dehydro org 2058-labelled receptor. Journal of Chromatography A. 1984 Aug 2;297:301-11.
