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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- No. CAS: 24320-06-7
- Fòrmula: C22H32O3
- Peso molecular:344.49
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Almacenamiento:
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Actividad biológica
Descripciòn
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progesterone receptor 1.25-1.68 nM (Kd) |
Bcl-2 |
Bcl-xL |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Normal human breast epithelial cells
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Concentration:100 nM
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Incubation Time:2; 3; 4; 5; 6 days
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Result:Inhibited the proliferation of normal human mammary epithelial cells.
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Cell Line:T47-D breast cancer cells
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Concentration:100 nM (alone); 10 nM E2 + 100 nM (combination)
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Incubation Time:3 days
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Result:Increased apoptosis to 160%.
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Cell Line:ZR75-1 breast cancer cells
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Concentration:100 nM
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Incubation Time:8 h; 48 h
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Result:Inhibited bcl-2 expression as soon as 8 hours after exposure, with a greater effect at 48 hours.
bcl-xL expression was decreased to 70% of control.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Baboon[1]
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Dosage:2.5 μg/kg body weight
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Administration:i.v.; single injection; 1 h
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Result:Nuclear uptake and retention were observed in secretory and stromal elements, with unlabeled cytoplasm.
Only 13.4% of alveolar secretory cells examined were labeled (n = 3816), while 60.2% of alveoli contained at least one labeled epithelial cell per cross-section (n = 260).
Individual secretory cells heavily concentrated radioactivity in their nuclei.
Most epithelial cells of interlobular ducts were labeled.
Fibroblasts of the interlobular connective tissue were heavily labeled, but fat cells were not labeled.
No cells of the intralobular connective tissue were labeled.
In the animal co-injected with unlabeled Progesterone, nuclear labeling in all aforementioned cell types was absent or significantly diminished.
Chemical Information
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No. CAS 24320-06-7
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Peso molecular 344.49
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Fòrmula C22H32O3
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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]
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ORG 2058 Related Classifications
HY-189016 Related Classifications
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