Size | Price | Stock | Qty |
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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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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Enzalutamide (formerly MDV3100; MDV-3100; trade name: Xtandi) is an orally bioavailable, 2nd-generation and non-steroidal androgen-receptor (AR) antagonist with potential antineoplastic activity. It inhibits AR with an IC50 of 36 nM in LNCaP cells. Enzalutamide belongs to the nonsteroidal antiandrogen (NSAA) class of medication and has been approve for treating prostate cancer. It has higher affinity to the AR compared to the first-generation AR inhibitors. It acts by blocking the binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA. The AR is a 919-amino acid member of the steroid receptor transcription factor superfamily with different domains including an N-terminal regulation domain.
ln Vitro |
Enzalutamide (MDV3100) in castration-resistant LNCaP/AR cells had a greater affinity for AR than ICI 176334 (AR-overexpressing) in a competitive assay using 16β-[18F]fluoro-5α-DHT (18-FDHT). On LNCaP/AR prostate cells, ezetimibe had no agonistic effects. Enzalutamide inhibits the activation of transmembrane serine protease 2 (TMPRSS2) and prostate-specific antigen (PSA) by binding to the synthetic androgen R1881, which is present in parental LNCaP cells. The transcriptional activity of the mutant AR protein (W741C, Trp741 altered to Cys) is inhibited by enzalutamide [1]. Additionally, enzalutamide inhibits the recruitment of coactivators and the nuclear translocation of ligand-receptor complexes [2].
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ln Vivo |
When administered at a dose of 10 mg/kg to castrated male mice harboring LNCaP/AR xenografts, enzalutamide (MDV3100) significantly reduces tumor growth [1]. The pharmacokinetics of enzalutamide show dose-independency when administered orally at dosages ranging from 0.5 to 5 mg/kg [4].
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Animal Protocol |
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References |
[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.
[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446. [3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305. [4]. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82 |
Molecular Formula |
C21H16F4N4O2S
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Molecular Weight |
464.44
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CAS # |
915087-33-1
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Related CAS # |
N-desmethyl Enzalutamide;1242137-16-1;N-desmethyl Enzalutamide-d6;Enzalutamide carboxylic acid;1242137-15-0;Deutenzalutamide-d3;1443331-82-5;Enzalutamide-d6;1443331-94-9
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SMILES |
S=C(N(C(C1(C)C)=O)C2=CC=C(C#N)C(C(F)(F)F)=C2)N1C3=CC(F)=C(C(NC)=O)C=C3
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Synonyms |
MDV-3100; MDV3100; MDV 3100; trade name: Xtandi.
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 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 (5.38 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. View More
Solubility in Formulation 3: 2.5 mg/mL (5.38 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 15% DMSO +85% PEG 300 : 10mg/mL Solubility in Formulation 5: 10 mg/mL (21.53 mM) in 1% Tween-80 in PBS (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1531 mL | 10.7657 mL | 21.5313 mL | |
5 mM | 0.4306 mL | 2.1531 mL | 4.3063 mL | |
10 mM | 0.2153 mL | 1.0766 mL | 2.1531 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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