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CX-5461 (dihydrochloride)
$120 – $880
Products Details
Product 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).
Web ID
– HY-13323A
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C27H29Cl2N7O2S
Citations
– 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.|Cancer Res. 2022 Jan 12;canres.1707.2021.|Cell Commun Signal. 2022 Sep 5;20(1):96.|Clin Cancer Res. 2017 Nov 1;23(21):6529-6540.|EMBO Mol Med. 2021 Mar 5;13(3):e12834.|FASEB J. 2020 Jun;34(6):8283-8295.|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.|Mol Cancer Ther. 2018 Jun;17(6):1177-1186.|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.|Nucleic Acids Res. 2022 May 6;50(8):4574-4600.|Oncotarget. 2017 Oct 29;8(57):96536-96552. |Patent. US20190169215A1
References
– [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.
Molecular Weight
– 586.54
Compound Purity
– 98.18
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
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– H2O : 5 mg/mL (ultrasonic;warming;heat to 80°C)
Target
– DNA/RNA Synthesis
Pathway
– Cell Cycle/DNA Damage
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
