Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
N-desmethyl Enzalutamide (N-desmethyl MDV 3100) is an active metabolite of Enzalutamide which is is a novel, potent, orally bioavailable, organic, non-steroidal small molecule, second-generation androgen-receptor (AR) antagonist. Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
ln Vivo |
Because it is more effective than enzalutamide and shows similar primary efficacy and secondary pharmacodynamics, N-Desmethylenzalutamide is an active adjuvant that may have a role in the clinical effects of enzalutamide. Enzalutamide's glucosamine metabolite is pharmacologically inert and has a circulating concentration that is roughly 25% less than enzalutamide's [1].
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References |
[1]. Gibbons JA, et al. Pharmacokinetic Drug Interaction Studies with Enzalutamide. Clin Pharmacokinet. 2015 Oct;54(10):1057-69.
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Molecular Formula |
C₂₀H₁₄F₄N₄O₂S
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Molecular Weight |
450.41
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CAS # |
1242137-16-1
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Related CAS # |
Enzalutamide;915087-33-1;N-desmethyl Enzalutamide-d6;Enzalutamide carboxylic acid;1242137-15-0
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SMILES |
S=C(N1C2=CC(F)=C(C(N)=O)C=C2)N(C3=CC=C(C(C(F)(F)F)=C3)C#N)C(C(C)1C)=O
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Synonyms |
N-desmethyl MDV 3100N-desmethyl MDV-3100N-desmethyl MDV3100
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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 (~222.02 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.55 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 (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2202 mL | 11.1010 mL | 22.2020 mL | |
5 mM | 0.4440 mL | 2.2202 mL | 4.4404 mL | |
10 mM | 0.2220 mL | 1.1101 mL | 2.2202 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.