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CX-4945 . hydrochloride

AG-CR1-3629-M001 1 mg INQ
AG-CR1-3629-M005 5 mg INQ
AG-CR1-3629-M025 25 mg INQ
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Additional Information

Product Data
Synonyms Silmitasertib . HCl; 8-Carboxy-N-(3-chlorophenyl)benzo[c][2,6] naphthyridin-5-aminium chloride
Properties
Formula C19H12ClN3O2 . HCl
MW 349.8 . 36.5
CAS 1009820-21-6 (free acid)
Purity ≥98%
Appearance Yellow solid.
Solubility Soluble in DMSO. Insoluble in water.
InChi Key OBOIGMDUOMSAHW-UHFFFAOYSA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
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Product Description

  • Orally active, potent and selective ATP-competitive inhibitor of the protein kinase CK2 (IC50=1nM).
  • Anticancer compound. Inhibits proliferation in a panel of cancer cell lines that overexpress CK2. Inhibited migration, blocks survival and induces apoptosis in cancer stem cells, glioblastomas and leukemia cells.
  • Shown to decrease the glucose metabolism in cancer cells.
  • Potent inhibitor of Cdc2-like kinases (Clks) in vitro, consequently interfering with alternative splicing.
  • Potent ATP-competitive inhibitor of DYRK1A (IC50=6.8nM), DYRK1B (IC50=6.4nM) and DYRK3 (IC50=18nM), involved in neurodegeneration-associated diseases.
  • CK2α deletion selectively increased M3 muscarinic receptors (M3Rs)-mediated insulin secretion from pancreatic islets.
  • Promoted cAMP-induced thermogenesis in white adipocytes.
  • CK2 inhibition ameliorates diet-induced obesity and insulin resistance in mice in vivo by promoting UCP1-dependent thermogenesis.

Product References

  1. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy: A. Siddiqui-Jain, et al.; Cancer Res. 70, 10288 (2010)
  2. Structural basis of CX-4945 binding to human protein kinase CK2: A.D. Ferguson, et al.; FEBS Lett. 585, 104 (2011)
  3. Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer: F. Pierre, et al.; J. Med. Chem. 54, 635 (2011)
  4. Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer: F. Pierre, et al.; Mol. Cell Biochem. 356, 37 (2011)
  5. CX-4945, a selective inhibitor of casein kinase-2 (CK2), exhibits anti-tumor activity in hematologic malignancies including enhanced activity in chronic lymphocytic leukemia when combined with fludarabine and inhibitors of the B-cell receptor pathway: R.C. Prins, et al.; Leukemia 27, 2094 (2013)
  6. CK2 inhibitor CX4945 induces sequential inactivation of proteins in the signaling pathways related with cell migration and suppresses metastasis of A549 human lung cancer cells: M.J. Ku, et al.; Bioorg. Med. Chem. Lett. 23, 5609 (2013)
  7. Identification of a novel function of CX-4945 as a splicing regulator: H. Kim, et al.; PLos One 9, e94978 (2014)
  8. Activity of the clinical-stage CK2-specific inhibitor CX-4945 against chronic lymphocytic leukemia: L.R. Martins, et al.; Leukemia 28, 179 (2014)
  9. Phosphoproteomics identifies CK2 as a negative regulator of beige adipocyte thermogenesis and energy expenditure: K. Shinoda, et al.; Cell Metab. 22, 997 (2015)
  10. CK2 acts as a potent negative regulator of receptor-mediated insulin release in vitro and in vivo: M. Rossi, et al.; PNAS 112, E6818 (2015)
  11. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies: H.J. Chon, et al.; Front. Pharmacol. 6, 70 (2015)
  12. A chemical with proven clinical safety rescues Down-syndrome-related phenotypes in through DYRK1A inhibition: H. Kim, et al.; Dis. Model Mech. 9, 839 (2016)
  13. Targeting protein kinase CK2 suppresses bladder cancer cell survival via the glucose metabolic pathway: X. Zhang, et al.; Oncotarget 7, 87361 (2016)
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