Molecular Weight(MW): 477.43
Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
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ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
J Cancer, 2014, 5(2):133-42.. Apalutamide (ARN-509) purchased from Selleck.
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Choose Selective Androgen Receptor Inhibitors
|Description||Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.|
ARN-509 (< 10 μM) inhibits androgen-mediated induction or repression of mRNA expression levels for 13 endogenous genes including PSA and TMPRSS2 in the LNCaP/AR prostate cancer cell line. ARN-509 (< 10 μM) inhibits the proliferative effect of R1881 (30 pM) in the LNCaP/AR prostate cancer cell line. ARN-509 (10 μM) impairs AR nuclear localization and thus reduces the concentration of AR available to bind androgen response elements (ARE) in LNCaP cells expressing AR-EYFP. ARN-509 (10 μM) is able to effectively compete with R1881 (1 nM) and prevent AR from binding to promoter regions. ARN-509 inhibits R1881-induced VP16-AR–mediated transcription with IC50 of 0.2 μM in Hep-G2 cells expressing a VP16-AR fusion protein and an ARE-driven luciferase reporter. 
|In vivo||ARN-509 (10 mg/kg/d, oral) inhibits tumor growth with decreased proliferative index and increased apoptotic rate in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dose dependently inhibits tumor growth with highest efficacy at dose of 30 mg/kg/day in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dosed at 10 mg/kg/d for 28 days results in a 3-fold reduction in prostates weight associated with lacking glandular secretory activity and 1.7-fold reduction in epididymis weight in adult male dogs. ARN-509 (10 mg/kg/d, oral) inhibits cell proliferation of prostate tissues in adult male dogs.  ARN-509 is safe and well tolerated in 24 patients with metastatic CRPC who has progressed on prior treatments and peak plasma concentrations occurred 2 to 3 hours after administration. ARN-509 results in durable PSA declines at doses ranging from 30 to 300 mg in patients with metastatic CRPC.  ARN-509 shows powerful anti-cancer activity and induces durable remissions long after therapy completion in castrate resistant prostate cancer mouse models. |
|In vitro||DMSO||18 mg/mL (37.7 mM)|
|Ethanol||5 mg/mL (10.47 mM)|
|In vivo||Add solvents to the product individually and in order:
0.5% CMC, pH4.0
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02949284||Not yet recruiting||Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma||Rutgers, The State University of New Jersey|National Cancer Institute (NCI)||June 2017||Phase 2|
|NCT02721979||Not yet recruiting||Stage II Prostate Adenocarcinoma||University of Washington|National Cancer Institute (NCI)||December 2016||Phase 2|
|NCT02770391||Recruiting||Prostate Cancer||Case Comprehensive Cancer Center||October 2016||Phase 2|
|NCT02849990||Not yet recruiting||Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer||University of Washington|National Cancer Institute (NCI)|Janssen Scientific Affairs, LLC||October 2016||Phase 2|
|NCT02772588||Recruiting||Prostate Cancer||Memorial Sloan Kettering Cancer Center|Janssen Pharmaceuticals|Weill Medical College of Cornell University|University of Michigan||May 2016||Phase 2|
|NCT02703623||Recruiting||Prostate Cancer||M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi||May 2016||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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