CX-5461

SKU: orb1306482

Description

CX5461 is an orally bioavailable small molecule that selectively inhibits RNA polymerase I, suppressing ribosomal RNA synthesis. This activity triggers a DNA damage response and demonstrates antitumor efficacy in preclinical models, including in vivo studies of ovarian cancer.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1138549-36-6
• MW: 513.61
• Purity: 99.40%
• Formula: C₂₇H₂₇N₇O₂S
• SMILES: CN1CCCN(CC1)c1ccc2c(n1)n1c3ccccc3sc1c(C(=O)NCc1cnc(C)cn1)c2=O
• Target: DNA/RNA Synthesis
• Solubility: H2O:5.15 mg/mL (10.03 mM);DMSO:1 mg/mL (1.95 mM)

Bioactivity

• Target IC50:
  Pol I-driven transcription of rRNA:142 nM
• In Vivo:
  In a mouse model of xenograft human solid tumors, oral administration of CX-5461 (50 mg/kg) demonstrated antitumor activity against solid tumors.
• In Vitro:
  METHODS: The phytopathogenic fungi A. tubingensis, Nigrospora oryzae and Phoma herbarum were treated with Carviolin (1-512 µg/mL) for 18 h and subjected to Antifungal Assay. RESULTS: Carviolin showed antifungal activity with MIC less than 200 µg/mL against all three fungi.
• Cell Research:
  Cells are plated on 96-well plates and treated the next day with dose response of CX-5461 for 96 hours. Cell viability is determined using Alamar Blue and CyQUANT assays(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, DNA Synthesis, DNA/RNA Synthesis, DNASynthesis, CX 5461, CX5461, CX-5461, RNASynthesis, RNA Synthesis, Pol I-driven transcription of rRNA

Compound Identifiers

PubChem CID

25257557