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Purity: ≥98%
Apalutamide (formerly JNJ56021927; ARN509; JNJ-56021927; ARN-509; trade name Erleada), an approved anticancer drug, is a potent, selective and competitive, orally bioavailable AR/androgen receptor inhibitor with an IC50 of 16 nM in a cell-free assay. In February 2018, Apalutamide received approval from FDA for the treatment of prostate cancer (non-metastatic castration-resistant PC-nmCRPC). Apalutamide is specifically indicated for use in conjunction with castration in the treatment of nmCRPC. The mechanism of action is to bind directly to the ligand-binding domain of the AR and block the effects of androgens.
| ln Vitro |
In radioligand binding experiments, aparalutamide (ARN-509) demonstrates a low micromolar affinity for GABAA receptors (IC50 3 μM), suggesting that it may potentially antagonize GABAA at levels that are inhibitory [1]. Strongly inhibiting the AR ligand-binding domain, apelutamide blocks the transcription of AR gene targets, DNA binding, and nuclear translocation of the androgen receptor (AR) [2].
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| ln Vivo |
Apalutamide (ARN-509) supports oral treatment once day in mice and dogs due to its long plasma half-life, excellent oral bioavailability, and low systemic clearance. The steady-state plasma levels of apalutamide rose in repeated dosing experiments, which is consistent with its extended terminal half-life. This led to high levels of C24 hours and a low peak-to-trough ratio (ratio: 2.5). Apalutamide at doses of 1, 10, or 30 mg/kg/day was administered to castrated male mice with LNCaP/AR xenograft tumors. On day 28, >50% tumor volume reduction was seen in 13 out of 20 animals treated with Apalutamide (30 mg/kg/day), compared to 19 out of 19 mice treated with MDV3100 (30 mg/kg/day). just 3[1].
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| References |
[1]. Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503.
[2]. Smith MR, et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838(16)30133 |
| Molecular Formula |
C21H15F4N5O2S
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|---|---|
| Molecular Weight |
477.43
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| CAS # |
956104-40-8
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| Related CAS # |
Apalutamide-d4;1638885-65-0;Apalutamide-d3;1638885-61-6;Apalutamide-13C,d3
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| SMILES |
O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F
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| Chemical Name |
4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide
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| Synonyms |
JNJ56021927; ARN509; JNJ-56021927; ARN 509; JNJ 56021927; ARN-509; Apalutamide; Brand name: Erleada
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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: ≥ 2.08 mg/mL (4.36 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 (4.36 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% CMC, pH4.0:14 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0945 mL | 10.4727 mL | 20.9455 mL | |
| 5 mM | 0.4189 mL | 2.0945 mL | 4.1891 mL | |
| 10 mM | 0.2095 mL | 1.0473 mL | 2.0945 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.
 ARN-509 activityin vitroin human prostate-cancer cells.Cancer Res.2012 Mar 15;72(6):1494-503. |
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 ARN-509impairs AR nuclear-localization and inhibits DNA-binding.Cancer Res.2012 Mar 15;72(6):1494-503. |
 ARN-509is active in models of castration-resistant prostate cancer.Cancer Res.2012 Mar 15;72(6):1494-503. |
 ARN-509achieves similar efficacy with lower steady-state plasma-levels than MDV3100 in LNCaP/AR xenograft models of castration-resistant prostate cancer.Cancer Res.2012 Mar 15;72(6):1494-503. |
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 ARN-509induces castrate-like changes in dog prostate and epididymis.Cancer Res.2012 Mar 15;72(6):1494-503. |
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