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| 5mg |
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11-Ketodihydrotestosterone (also known as 11-KDHT; 5α-Dihydro-11-keto testosterone), an endogenous steroid, is a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a highly potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
| ln Vitro |
Treatment of LNCaP and VCaP cells with 11-ketodihydrotestosterone (11-KDHT; 1–10 nM; 24 hours) causes a notable induction of cell proliferation [1]. With the exception of 1 nM of KLK3 in LNCaP cells, treatment with 11-ketodihydrotestosterone (11-KDHT; 0.1-10 nM; 7-10 days; LNCaP and VCaP cells) significantly upregulated the expression of KLK3, TMPRSS2, and FKBP5. Merely 20% of 11β-hydroxyandrostenedione (11OHA4) and 11β-hydroxytestosterone (11OHT) are metabolized in PNT2 cells. The former generates 11-keto-androstenedione (11KA4), 11-ketodihydrotestosterone (11-KDHT), and 11β-hydroxy-5α-androstanedione (11OH-5αDIONE), while the latter yields 11OHA4, 11KT, and 11-ketodihydrotestosterone, with downstream products <0.03 μM [2]. C11-oxoC19 metabolites were found in prostate cancer tissue at much higher concentrations than C19 steroids; unconjugated 11-ketodihydrotestosterone, 11KT, and 11OHA4 levels ranged from 13 to 37.5 ng/g. Significant quantities of 11OHA4 (about 230-440 nM), 11KT (approximately 250-390 nM), and 11-ketodihydrotestosterone (approximately 19 nM) were found in plasma when total steroid levels were analyzed [2].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: LNCaP and VCaP cells Tested Concentrations: 0.1 nM, 1 nM or 10 nM Incubation Duration: 7 days (LNCaP cells) or 10 days (VCaP cells) Experimental Results: Significant cell proliferation was induced. RT-PCR[1] Cell Types: LNCaP and VCaP Cell Tested Concentrations: 1 nM, 10 nM Incubation Duration: 24 hrs (hours) Experimental Results: Result in significant upregulation of KLK3, TMPRSS2 and FKBP5 in LNCaP (Figure 3) and VCaP (Figure 4) cells . |
| References |
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| Molecular Formula |
C19H28O3
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|---|---|
| Molecular Weight |
304.423826217651
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| Exact Mass |
304.203
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| CAS # |
32694-37-4
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| Related CAS # |
11-Ketodihydrotestosterone-d3;2479914-02-6
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| PubChem CID |
11197479
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
453.4±45.0 °C at 760 mmHg
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| Flash Point |
242.1±25.2 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.546
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| LogP |
1.84
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
22
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| Complexity |
527
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@]12CCC(=O)C[C@@H]1CC[C@@H]3[C@@H]2C(=O)C[C@]4([C@H]3CC[C@@H]4O)C
|
| InChi Key |
RSQKILYTRHKUIJ-HZGXJFKTSA-N
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| InChi Code |
InChI=1S/C19H28O3/c1-18-8-7-12(20)9-11(18)3-4-13-14-5-6-16(22)19(14,2)10-15(21)17(13)18/h11,13-14,16-17,22H,3-10H2,1-2H3/t11-,13-,14-,16-,17+,18-,19-/m0/s1
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| Chemical Name |
(5S,8S,9S,10S,13S,14S,17S)-17-hydroxy-10,13-dimethyl-2,4,5,6,7,8,9,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,11-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~328.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.21 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2849 mL | 16.4247 mL | 32.8494 mL | |
| 5 mM | 0.6570 mL | 3.2849 mL | 6.5699 mL | |
| 10 mM | 0.3285 mL | 1.6425 mL | 3.2849 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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