| Chemical Properties | Back Directory | [Boiling point ]
822.4±65.0 °C(Predicted) | [density ]
1.321±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
9.86±0.20(Predicted) | [color ]
Brown to dark brown |
| Hazard Information | Back Directory | [Description]
CM03 is a potent inhibitor of cell growth in PDAC cell lines, and has anticancer activity in PDAC models, with a superior profile compared to gemcitabine, a commonly used therapy. Whole-transcriptome RNA-seq methodology has been used to analyze the effects of this quadruplexbinding small molecule on global gene expression. This has revealed the down-regulation of a large number of genes, rich in putative quadruplex elements and involved in essential pathways of PDAC survival, metastasis, and drug resistance. The changes produced by CM03 represent a global response to the complexity of human PDAC and may be applicable to other currently hard-to-treat cancers. | [Uses]
CM03 is a potent DNA G-quadruplexes (G4s) ligand. CM03 can stabilise G4s, downregulating more G4-containing genes as well as increasing incidence of double-strand break events (DSBs) due to torsional strain on DNA and chromatin structure. CM03 has selective potency for pancreatic cancer cells[1][2]. | [References]
[1] Ahmed AA, et al. A G-Quadruplex-Binding Small Molecule and the HDAC Inhibitor SAHA (Vorinostat) Act Synergistically in Gemcitabine-Sensitive and Resistant Pancreatic Cancer Cells. Molecules. 2020 Nov 19;25(22):5407. DOI:10.3390/molecules25225407
[2] Ahmed AA, et al. Asymmetrically Substituted Quadruplex-Binding Naphthalene Diimide Showing Potent Activity in Pancreatic Cancer Models. ACS Med Chem Lett. 2020 Jul 16;11(8):1634-1644. DOI:10.1021/acsmedchemlett.0c00317 |
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