CX-5461

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    CX-5461 is a potent and orally bioavailable small-molecule inhibitor of rRNA synthesis that specifically inhibits RNA polymerase (Pol) I-driven transcription with IC50 value of 142 nM. CX-5461 exhibits antiproliferative activity against human pancreatic tumor cells MIA Paca-2, human melanoma cells A375 and colorectal carcinoma cells HCT-116 with EC50 values of 74, 58, and 167 nmol/L, respectively. [1].
    CX-5461 was revealed to inhibit Pol I transcription via promoting the stabilization of p53. In addition, CX-5461 has been demonstrated to induce autophagy and senescence but not apoptosis in MIA Paca-2 and A375 cell lines.
    In vivo, CX-5461 has shown to suppress tumor volume in both MIA Paca-2 and A375 derived xenograft mice models [1].
    
    [1] Drygin D1, Lin A, Bliesath J, Ho CB, O'Brien SE, Proffitt C, Omori M, Haddach M, Schwaebe MK, Siddiqui-Jain A, Streiner N, Quin JE, Sanij E, Bywater MJ,Hannan RD, Ryckman D, Anderes K, Rice WG. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 2011 Feb 15;71(4):1418-30
- Properties
  - Alternative Name
    
    CX 5461;CX5461; 2-(4-methyl-1,4-diazepan-1-yl)-N-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
    
    CAS Number
    
    1138549-36-6
    
    Molecular Formula
    
    C27H27N7O2S
    
    Molecular Weight
    
    513.61
    
    Appearance
    
    A solid
    
    Purity
    
    98.34%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; insoluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zonneville J, Wong V, et al. "TAK1 signaling regulates p53 through a mechanism involving ribosomal stress." Sci Rep. 2020 Feb 13;10(1):2517. PMID:32054925
    2.Rossetti S, Wierzbicki AJ, et al. "Undermining ribosomal RNA transcription in both the nucleolus and mitochondrion: an offbeat approach to target MYC-driven cancer." Oncotarget. 2017 Dec 22;9(4):5016-5031. PMID:29435159
    3.Rossetti S, Wierzbicki AJ, et al. "Mammary epithelial morphogenesis and early breast cancer. Evidence of involvement of basal components of the RNA Polymerase I transcription machinery." Cell Cycle. 2016 Aug 2:0. PMID:27485818

CX-5461

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