CX-5461
CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively[1].
Product Specifications
CAS Number
1138549-36-6
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
DNA/RNA Synthesis
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/cx-5461.html
Purity
99.50
Solubility
50 mM Sodium phosphate (pH 3.5) : 10 mg/mL (ultrasonic) |DMSO : < 1 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : 55.56 mg/mL (ultrasonic; adjust pH to 2 with HCl)
Smiles
CC1=NC=C(CNC(C2=C3N(C4=NC(N5CCN(CCC5)C)=CC=C4C2=O)C6=C(S3)C=CC=C6)=O)N=C1
Molecular Formula
C27H27N7O2S
Molecular Weight
513.61
Precautions
H302, H315, H319, H335
References & Citations
[1]Drygin D et al. 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.|[2]Bywater MJ, et al. Inhibition of RNA Polymerase I as a Therapeutic Strategy to Promote Cancer-Specific Activation of p53.
 Cancer Cell. 2012 Jul 10;22 (1) :51-65.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Citation 01
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