851983-85-2
Galeterone
CAS: 851983-85-2
Molecular Formula: C26H32N2O
851983-85-2 - Names and Identifiers
851983-85-2 - Physico-chemical Properties
| Molecular Formula | C26H32N2O |
| Molar Mass | 388.55 |
| Density | 1.28 |
| Melting Point | 189-190℃ |
| Boling Point | 564.5±60.0 °C(Predicted) |
| Solubility | Chloroform (Slightly), Ethyl Aceatae (Slightly, Heated) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 14.71±0.70(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | Galeterone is an effective pre-blocking [. In PC3 cells, Galeterone also inhibits [. Galeterone potently inhibited the proliferation of androgen-independent cell lines PC - 3 and DU-145 in a dose-dependent manner with GI50 of 7.82 μm and 7.55 μm, respectively. The endoplasmic reticulum stress response induced by Galeterone results in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA. Galeterone effectively inhibited HP-LNCaP and C4-2B proliferation with IC 50 of 2.9 μm and 9.7 μm, respectively. 1 μm Galeteron effectively inhibited androgen receptor activation, with inhibition rates of 50% in LNCaP and 70% in HP-LNCaP. In LNCaP cells and HP-LNCaP cells, Galeterone reduced androgen receptor activation with IC 50 of 1 μm and 411 nM, respectively, and down-regulated androgen receptor protein expression by 50% after 24-h treatment. Galeterone reduces AR protein and mRNA expression, antagonizes androgen-induced AR-dependent promoter activation, and significantly reduces phosphorylated -4EBP1 levels |
| In vivo study | Administration of Galeterone at a dose of 50 mg/kg (twice daily) was highly effective in inhibiting xenografts of the growth hormone-dependent human prostate tumor LAPC4 compared with controls, the final tumor volume was reduced by 93.8%, and the effectiveness was significantly higher than that of castration. Treatment with Galeterone at 0.13 mm/kg, or 0.13mmol/kg twice daily, combined with castration reduced LAPC4 xenograft tumors by 26.55 and 60.67 percent in SCID mice. Treatment with Galeterone alone or plus castration significantly reduced AR protein expression by 10-and 5-fold. |
851983-85-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.574 ml | 12.868 ml | 25.736 ml |
| 5 mM | 0.515 ml | 2.574 ml | 5.147 ml |
| 10 mM | 0.257 ml | 1.287 ml | 2.574 ml |
| 5 mM | 0.051 ml | 0.257 ml | 0.515 ml |
Last Update：2024-01-02 23:10:35
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CAS: 851983-85-2
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CAS: 851983-85-2
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Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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