ARN-509

CAS No. 956104-40-8

ARN-509( JNJ-56021927 )

Catalog No. M16822 CAS No. 956104-40-8

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate Y treatment.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 43 In Stock
5MG 65 In Stock
10MG 113 In Stock
25MG 239 In Stock
50MG 340 In Stock
100MG 535 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    ARN-509
  • Note
    Research use only, not for human use.
  • Brief Description
    ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate Y treatment.
  • Description
    ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate Y treatment. Phase 3.(In Vitro):Apalutamide (ARN-509) also exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor in radioligand binding-assays and thus may potentially antagonize GABAA at therapeutic dose levels. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets.(In Vivo):Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability and long plasma half-life in both mouse and dog, supporting once-daily oral dosing. Consistent with its long terminal-half-life, Apalutamide steady-state plasma-levels increases in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (ratio:2.5). Castrate male mice bearing LNCaP/AR xenograft tumors are treated with either Apalutamide at doses of 1, 10 or 30 mg/kg/day. Thirteen of 20 Apalutamide (30 mg/kg/day)-treated animals exhibit >50% reduction in tumor-volume at day 28 versus 3 of 19 MDV3100 (30 mg/kg/day)-treated mice.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    JNJ-56021927
  • Pathway
    Endocrinology/Hormones
  • Target
    Androgen Receptor (AR)
  • Recptor
    Androgen Receptor| GABAR
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    956104-40-8
  • Formula Weight
    477.43
  • Molecular Formula
    C21H15F4N5O2S
  • Purity
    >98% (HPLC)
  • Solubility
    Ethanol: 5 mg/mL (10.47 mM); DMSO: 18 mg/mL (37.7 mM)
  • 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
  • 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Clegg NJ, et al. Y Res, 2012, 72(6), 1494-1503.
molnova catalog
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