CX-5461 (dihydrochloride)
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM) .
Product Specifications
UNSPSC
12352005
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-5416_HCl.html
Purity
99.41
Solubility
H2O : 5 mg/mL (ultrasonic; warming; heat to 80°C)
Smiles
[H]Cl.CC1=NC=C(CNC(C2=C3N(C4=NC(N5CCN(CCC5)C)=CC=C4C2=O)C6=C(S3)C=CC=C6)=O)N=C1.[H]Cl
Molecular Formula
C27H29Cl2N7O2S
Molecular Weight
586.54
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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Citation 01
BioRxiv. 2023 Jan 31.|Int J Biol Macromol. 2025 Sep;322 (Pt 1) :146723.|Sci Adv. 2023 Sep;9 (35) :eadg7125.|Acta Biomater. 2018 Oct 1:79:317-330.|Am J Pathol. 2021 Jun;191 (6) :1094-1107.|Anal Chem. 2025 Jun 10;97 (22) :11617-11626.|Biochim Biophys Acta. 2017 Dec 8;1862 (3) :615-629.|Biochimie. 2022 Apr 20;199:81-91.|Biomed Pharmacother. 2021 Jan;133:110906.|bioRxiv. 2021 Dec.|bioRxiv. 2024 November 28.|bioRxiv. 2024 October 13.|bioRxiv. 2024 Sep 29:2024.09.28.615444.|bioRxiv. 2025 Aug 19.|bioRxiv. 2025 January 21.|bioRxiv. 2025 Jul 23.|bioRxiv. 2025 May 10.|bioRxiv. 2025 Nov 20:2025.11.19.689351.|Cancer Res. 2022 Mar 15;82 (6) :1013-1024.|Cell Commun Signal. 2022 Sep 5;20 (1) :96.|Cell Death Dis. 2024 Mar 29;15 (3) :236.|Cell Death Dis. 2025 Nov 7;16 (1) :812.|Cell Prolif. 2025 May 4:e70052.|Cell Signal. 2025 Nov:135:111998.|Cell. 2024 Mar 28;187 (7) :1701-1718.e28.|Clin Cancer Res. 2017 Nov 1;23 (21) :6529-6540.|Development. 2024 Nov 1;151 (21) :dev202875.|EMBO Mol Med. 2021 Mar 5;13 (3) :e12834.|Eur J Med Chem Rep. 2025 Dec.|Eur J Pharmacol. 2025 Sep 15:1003:177942.|Exp Cell Res. 2025 Jun 2;450 (2) :114629.|FASEB J. 2020 Jun;34 (6) :8283-8295.|Free Radic Biol Med. 2024 Aug 5:S0891-5849 (24) 00589-6.|Harvard Medical School LINCS LIBRARY|Int J Biol Macromol. 2025 May 15:144179.|Invest New Drugs. 2021 Oct;39 (5) :1213-1221.|J Cell Biol. 2023 Jan 2;222 (1) :e202202110.|J Extracell Vesicles. 2023 Oct;12 (10) :e12361.|J Transl Med. 2024 Dec 25;22 (1) :1147.|Life Sci Alliance. 2019 Feb 26;2 (2) :e201800222.|Matrix Biol. 2024 Dec:134:93-106.|Mol Cancer Ther. 2018 Jun;17 (6) :1177-1186.|Mol Cancer. 2024 Dec 20;23 (1) :275.|Mol Cell. 2025 Sep 18;85 (18) :3425-3442.e10.|Mol Ther Oncol. 2024 Feb 7;32 (1) :200771.|Molecules. 2019 Dec 4;24 (24) :4445.|Nat Cell Biol. 2022 Jul;24 (7) :1154-1164.|Nat Commun. 2017 Sep 25;8 (1) :693. |Nat Commun. 2022 Jun 28;13 (1) :3706.|Nat Commun. 2024 Feb 9;15 (1) :1231.|Nat Commun. 2025 Jan 2;16 (1) :121.|Nat Commun. 2025 Jan 4;16 (1) :390.|Nat Commun. 2025 Jul 14;16 (1) :6489.|Nature. 2025 Aug;644 (8076) :557-566.|Nucleic Acids Res. 2022 May 6;50 (8) :4574-4600.|Oncotarget. 2017 Oct 29;8 (57) :96536-96552. |Open Biol. 2025 Feb;15 (2) :240183.|Patent. US20190169215A1|Science. 2025 Nov 13:eadz3121.|Tissue Cell. 2025 Aug 18:97:103093.|Utrecht University. 2023 Feb.
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