Apalutamide

SKU: orb1305642

Description

Apalutamide

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 956104-40-8
• MW: 477.43
• Purity: 99.97% (May vary between batches)
• Formula: C₂₁H₁₅F₄N₅O₂S
• SMILES: CNC(=O)c1ccc(cc1F)N1C(=S)N(C(=O)C11CCC1)c1cnc(C#N)c(c1)C(F)(F)F
• Target: Androgen Receptor|||GABA Receptor
• Solubility: DMSO:240 mg/mL (502.69 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.47 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:5 mg/mL (10.47 mM)

Bioactivity

• Target IC50:
  Androgen receptor:16 nM
• In Vivo:
  At a concentration of 10 μM, ARN-509 disrupts the nuclear localization of AR in LNCaP cells expressing AR-EYFP, resulting in a decreased concentration of AR available for binding to androgen response elements (ARE) in cells expressing AR-EYFP. ARN-509 also inhibits R1881-induced transcription mediated by VP16-AR fusion protein in Hep-G2 cells expressing VP16-AR fusion protein and an ARE-driven luciferase reporter, with an IC50 value of 0.2 μM. Furthermore, ARN-509 (at concentrations <10 μM) suppresses the androgen-mediated induction or repression of mRNA expression levels of 13 endogenous genes (including PSA and TMPRSS2) in the LNCaP/AR prostate cancer cell line. Moreover, in the LNCaP/AR prostate cancer cell line, ARN-509 (<10 μM) inhibits the proliferative effects of R1881 (30 pM). At the concentration of 10 μM, ARN-509 effectively competes with 1 nM R1881, thereby preventing AR from binding to promoter regions.
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• In Vitro:
  Administering 10 mg/kg of ARN-509 orally daily inhibits cell proliferation in the prostate tissue of adult male dogs. In castrated male immunodeficient mice with LNCaP/AR-luc xenograft tumors, ARN-509 (10 mg/kg/day, orally) suppresses tumor growth, decreases the proliferation index, and increases apoptosis rates. This compound demonstrates a dose-dependent inhibition of tumor growth in castrated male immunodeficient mice carrying LNCaP/AR-luc xenograft tumors. A 28-day administration of ARN-509 at 10 mg/kg/day results in a lack of glandular secretory activity and a 1.7-fold reduction in epididymal weight in adult male dogs, associated with a threefold decrease in prostate weight. In patients with metastatic CRPC, ARN-509 induces a sustained decline in PSA levels within the 30 to 300 mg range. ARN-509 exhibits strong anticancer activity in castrated anti-prostate cancer mouse models, inducing prolonged symptom relief after treatment completion. It is safe and well-tolerated in 24 patients with metastatic CRPC who have undergone prior treatments, with peak plasma levels appearing 2 to 3 hours post-administration.
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• Cell Research:
  Cells are incubated for 48 hours, after which ARN-509 is added in a 16 μL volume to the RPMI culture medium. For the antagonist mode assay, the ARN-509 is diluted in culture medium also containing 30 pM R1881. After 7 days' incubation, 16 μL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apalutamide, Androgen Receptor, AndrogenReceptor, ARN509, ARN-509, ARN 509, GABA Receptor, GABAReceptor, GABAR, inhibit, Inhibitor

Compound Identifiers

PubChem CID

24872560