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VPC 14449

CAS No. 1621375-32-3

VPC 14449( VPC14449 )

Catalog No. M12386 CAS No. 1621375-32-3

VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    VPC 14449
  • Note
    Research use only, not for human use.
  • Brief Description
    VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM.
  • Description
    VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression; effectively blocks transcriptional activity of full-length and splice variant AR forms at low to sub-micromolar concentrations; reduces tumor volume and abolishes PSA production in LNCaP xenograft model.
  • In Vitro
    Cell Viability Assay Cell Line:LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration:0.01, 0.1, 10, 100 μM Incubation Time:24 hours Result:Suppressed the growth of every tested cell line.Western Blot Analysis Cell Line:LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration:0.01, 0.1, 10, 100 μM Incubation Time:24 hours Result:Inhibited endogenous AR transactivation in LNCaP, C4-2 and MR49F cells stimulated with the synthetic androgen R1881.
  • In Vivo
    Animal Model:Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated Dosage:100 mg/kg Administration:I.p. twice daily for 4 weeks Result:Suppressed LNCaP tumor volume and blocked serum PSA production.
  • Synonyms
    VPC14449
  • Pathway
    Endocrinology/Hormones
  • Target
    Androgen Receptor (AR)
  • Recptor
    Androgen Receptor (AR)
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1621375-32-3
  • Formula Weight
    394.085
  • Molecular Formula
    C10H10Br2N4OS
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 125 mg/mL (317.19 mM)
  • SMILES
    BrC1=C(Br)N=CN1C2=CSC(N3CCOCC3)=N2
  • Chemical Name
    4-(4-(4,5-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine

Shipping & Storage Information

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

Reference

1. Dalal K, et al. Mol Cancer Ther. 2017 Aug 3. pii: molcanther.0259.2017. 2. Dalal K, et al. J Biol Chem. 2014 Sep 19;289(38):26417-29.
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