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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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Enzalutamide carboxylic acid (also called MDV-3100 carboxylic acid) is a major inactive metabolite of Enzalutamide (MDV3100; Xtandi) which is a non-steroidal androgen-receptor (AR) antagonist approved for use as an anticancer drug.
ln Vitro |
By means of cytochrome P450 (CYP) 3A4/5 and CYP2C8, enzalutamide is transformed into its principal metabolites, N-desmethylenzalutamide and enzalutamide carboxylate, respectively. While enzalutamide carboxylate is inactive, N-desmethylenzalutamide exhibits clinically significant antiandrogenic activity that is comparable to enzalutamide [1].
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References |
[1]. van Nuland M, et al. Exposure-Response Assessment of Enzalutamide and Its Major Metabolites in a Real-World Cohort of Patients with Metastatic Castration-Resistant Prostate Cancer. Pharmacotherapy. 2019 Dec;39(12):1137-1145.
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Molecular Formula |
C₂₀H₁₃F₄N₃O₃S
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Molecular Weight |
451.39
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CAS # |
1242137-15-0
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Related CAS # |
Enzalutamide;915087-33-1;N-desmethyl Enzalutamide;1242137-16-1;Enzalutamide carboxylic acid-d6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC1(C)C(=O)N(C2=CC(=C(C=C2)C#N)C(F)(F)F)C(=S)N1C3=CC(=C(C=C3)C(=O)O)F
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Synonyms |
Enzalutamide carboxylic acidMDV3100 carboxylic acidMDV-3100 carboxylic acid
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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 : ~125 mg/mL (~276.92 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.61 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 20.8 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: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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: ≥ 2.08 mg/mL (4.61 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 | 2.2154 mL | 11.0769 mL | 22.1538 mL | |
5 mM | 0.4431 mL | 2.2154 mL | 4.4308 mL | |
10 mM | 0.2215 mL | 1.1077 mL | 2.2154 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.