CX-5461 (dihydrochloride)

CX-5461 (dihydrochloride)

• UNSPSC Description: 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).
• Target Antigen: DNA/RNA Synthesis
• Type: Reference compound
• Related Pathways: Cell Cycle/DNA Damage
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/CX-5416_HCl.html
• 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 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.bioRxiv. 2023 Jan 31.|Sci Adv. 2023 Sep;9(35):eadg7125.|Acta Biomater. 2018 Oct 1;79:317-330.|Am J Pathol. 2021 Mar 8;S0002-9440(21)00084-5.|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.|Cancer Res. 2022 Jan 12;canres.1707.2021.|Cell Commun Signal. 2022 Sep 5;20(1):96.|Cell Death Dis. 2024 Mar 29;15(3):236.|Cell. 2024 Mar 28;187(7):1701-1718.e28.|Clin Cancer Res. 2017 Nov 1;23(21):6529-6540.|Development. 2024 Sep 26:dev.202875.|EMBO Mol Med. 2021 Mar 5;13(3):e12834.|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|Invest New Drugs. 2021 Mar 12.|J Cell Biol. 2023 Jan 2;222(1):e202202110.|J Extracell Vesicles. 2023 Oct;12(10):e12361.|Life Sci Alliance. 2019 Feb 26;2(2):e201800222.|Matrix Biol. 2024 Oct 5:S0945-053X(24)00124-0.|Mol Cancer Ther. 2018 Jun;17(6):1177-1186.|Mol Cancer. 2024 Dec 20;23(1):275.|Molecular Therapy Oncology. 2024 Feb 7.|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.|Nucleic Acids Res. 2022 May 6;50(8):4574-4600.|Oncotarget. 2017 Oct 29;8(57):96536-96552. |Patent. US20190169215A1|Utrecht University. 2023 Feb.
• Shipping Conditions: Room Temperature