Silmitasertib (sodium salt)

• UNSPSC Description:

  Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.

• Target Antigen:

  Autophagy; Casein Kinase

• Type:

  Reference compound

• Related Pathways:

  Autophagy;Cell Cycle/DNA Damage;Stem Cell/Wnt

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/CX-4945-sodium-salt.html

• Purity:

  99.92

• Solubility:

  DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : 16.67 mg/mL (ultrasonic)

• Smiles:

  O=C(C1=CC=C2C3=C(C(NC4=CC=CC(Cl)=C4)=NC2=C1)C=CN=C3)O[Na]

• Molecular Weight:

  371.75

• References & Citations:

  [1]Siddiqui-Jain A, et al. CX-4945, an orally bioavailable selective inhibitor of protein kinase CK2, inhibits prosurvival and angiogenic signaling and exhibits antitumor efficacy. Cancer Res. 2010 Dec 15;70(24):10288-98.|[2]Buontempo F, et al. Synergistic cytotoxic effects of PS-341 and CK2 inhibitor CX-4945 in acute lymphoblastic leukemia: turning off the prosurvival ER chaperone BIP/Grp78 and turning on the pro-apoptotic NF-κB. Oncotarget. 2016 Jan 12;7(2):1323-40.|[3]Chon HJ, et al. The casein kinase 2 inhibitor, CX-4945, as an anti-cancer drug in treatment of human hematological malignancies. Front Pharmacol. 2015 Mar 31;6:70.|[4]Kendall JJ, et al. CK2 blockade causes MPNST cell apoptosis and promotes degradation of β-catenin. Oncotarget. 2016 Aug 16;7(33):53191-53203.Int J Mol Sci. 2021 Jan 15;22(2):E819.|Oncotarget. 2016 Aug 16;7(33):53191-53203.|Autophagy. 2024 Aug 22.|Biochem Biophys Res Commun. 2020 Oct 20;531(3):409-415.|Biomed Pharmacother. 2024 Jul 29:178:117191.|bioRxiv. 2023 Oct 23.|bioRxiv. 2024 Jul 25:2024.07.25.605073.|bioRxiv. 2024 Nov 6:2024.11.04.621884.|Cancers (Basel). 2021, 13(5), 1127.|Cell Death Dis. 2024 Mar 16.|Cell Death Discov. 2024 Apr 22;10(1):185.|Cell Mol Biol Lett. 2023 Oct 24;28(1):85.|Cell Rep Methods. 2023 Oct 23;3(10):100599.|Cell Rep. 2023 Apr 3;42(4):112339.|Cell Stem Cell. 2023 Apr 6;30(4):450-459.e9.|Cells. 2021 Jan 18;10(1):E181.|Drug Res (Stuttg). 2024 Mar 20.|Electronic Theses and Dissertations. 2023 Jul.|EMBO Mol Med. 2020 Aug 7;12(8):e11987.|Heliyon. 2024 Aug 18;10(16):e36205.|Int J Mol Sci. 2020 Mar 3;21(5):1718. |Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14.|J Biol Chem. 2024 Sep 30:107848.|J Immunol. 2023 Mar 27;ji2200598.|J Med Chem. 2023 Mar 6.|J Med Chem. 2023 Mar 8.|Nat Cell Biol. 2021 Mar;23(3):257-267.|Nat Commun. 2023 Feb 9;14(1):731.|Nat Commun. 2024 Oct 16;15(1):8912.|Oncogene. 2017 Aug 24;36(34):4943-4950.|Oncogene. 2022 Jan;41(4):571-585.|Oncol Rep. 2017 Feb;37(2):1141-1147. |Patent. US20180263995A1.|Research Square Preprint. 2023 May 26.|Research Square Preprint. 2023 Oct 27.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Science. 2017 Dec 1;358(6367):eaan4368.|Signal Transduct Target Ther. 2023 May 10;8(1):183.|University of California. 2023 Feb.|University of Concepcion. 2023.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  Phase 2

• CAS Number:

  1309357-15-0