11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) 是一种内源性类固醇，是 11β-羟基雄烯二酮的代谢产物。11-Ketodihydrotestosterone 是一种活性雄激素，也是一种有效的雄激素受体 (AR) 激动剂，对人AR的Ki为 20.4 nM，EC50为 1.35 nM。11-Ketodihydrotestosterone 在雄激素依赖性前列腺癌细胞中诱导基因调节，蛋白质表达和细胞生长。
| 生物活性 | 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potentandrogen receptor(AR)agonist with aKiof 20.4 nM and anEC50of 1.35 nM forhuman AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostatecancercells[1][2]. |
| IC50& Target | Ki: 20.4 nM (Human androgen receptor)[1]
EC50: 1.35 nM (Human androgen receptor)[1] |
体外研究
(In Vitro) | 11-Ketodihydrotestosterone (11-KDHT; 1-10 nM; 24 hours; LNCaP and VCaP cells) treatment induces significant cell proliferation[1].
11-Ketodihydrotestosterone (11-KDHT; 0.1-10 nM; 7-10 days; LNCaP and VCaP cells) treatment results in the significant upregulation ofKLK3,TMPRSS2andFKBP5in both LNCaP and VCaP cells, with the exception ofKLK3at 1 nM in LNCaP cells[1].
In PNT2 cells, only 20% of 11β-hydroxyandrostenedione (11OHA4) and 11β-hydroxytestosterone (11OHT) are metabolised with the former yielding 11keto-androstenedione (11KA4), 11-Ketodihydrotestosterone (11-KDHT) and 11β-hydroxy-5α-androstanedione (11OH-5αDIONE) and the latter yielding 11OHA4, 11KT and 11-Ketodihydrotestosterone with downstream products<0.03 μM[2].
In prostate cancer tissue, C11-oxy C19 metabolites at significantly higher levels than the C19 steroids are detected, with unconjugated 11-Ketodihydrotestosterone, 11KT and 11OHA4 levels ranging between 13 and 37.5 ng/g. Analyses of total steroid levels in plasma show significant levels of 11OHA4 (≈230-440 nM), 11KT (≈250-390 nM) and 11-Ketodihydrotestosterone (≈19 nM)[2].
Cell Proliferation Assay[1] | Cell Line: | LNCaP and VCaP cells | | Concentration: | 0.1 nM, 1 nM or 10 nM | | Incubation Time: | 7 days (LNCaP cells) or 10 days (VCaP cells) | | Result: | Induced significant cell proliferation. |
RT-PCR[1] | Cell Line: | LNCaP and VCaP cells | | Concentration: | 1 nM, 10 nM | | Incubation Time: | 24 hours | | Result: | Resulted in the significant upregulation ofKLK3,TMPRSS2andFKBP5in both LNCaP (Fig 3) and VCaP (Fig 4) cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(328.49 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.2849 mL | 16.4247 mL | 32.8493 mL | | 5 mM | 0.6570 mL | 3.2849 mL | 6.5699 mL | | 10 mM | 0.3285 mL | 1.6425 mL | 3.2849 mL |
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此方案可获得 ≥ 2.5 mg/mL (8.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (8.21 mM); Suspended solution; Need ultrasonic
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