Ceritinib

• UNSPSC Description:

  Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency[1][2].

• Target Antigen:

  Anaplastic lymphoma kinase (ALK); IGF-1R; Insulin Receptor

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer; Endocrinology

• Assay Protocol:

  https://www.medchemexpress.com/LDK378.html

• Solubility:

  DMSO : 12.5 mg/mL (ultrasonic;warming;heat to 60°C)

• Smiles:

  CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3

• Molecular Weight:

  558.14

• References & Citations:

  [1]Marsilje TH, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90.|[2]Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4.|[3]Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006.|[4]Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81.AMB Express. 2022 Nov 28;12(1):150.|Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867(7):118712.|Cancer Chemother Pharmacol. 2018 Aug;82(2):251-263.|Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.|Cell Discov. 2021 May 11;7(1):33.|Cell Physiol Biochem. 2018;45(4):1707-1716.|Cell Rep Med. 2023 Jan 10;100911.|Cell Signal. 2022 Jan 24;92:110264.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Eur J Med Chem. 2022: 114946.|Fundam Clin Pharmacol. 2021 Feb 1.|Harvard Medical School LINCS LIBRARY|J Med Chem. 2024 Oct 3.|J Pharm Pharmacol. 2020 Oct;72(10):1370-1382.|J Transl Med. 2021 Feb 27;19(1):91.|Mol Oncol. 2017 Aug;11(8):996-1006.|Mol Syst Biol. 2023 Dec 18.|Nat Cancer. 2022 Oct;3(10):1211-1227.|Nat Commun. 2024 Apr 23;15(1):3422.|Patent. US20200276189A1.|Patent. US20230158019A1.|RSC Adv. 2023 Mar 10;13(12):7929-7938.|Sci Signal. 2015 Dec 8;8(406):ra125. |Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Science. 2017 Dec 1;358(6367):eaan4368.|Toxicol Appl Pharmacol. 2019 Nov 15;383:114781.|Universitat Autònoma de Barcelona. Biologia Molecular i Biomedicina. 2022 Aug.|Uppsala University. Department of Pharmaceutical Biosciences. 2022 Feb.|Xenobiotica. 2018 Oct;48(10):1059-1071. |bioRxiv. 2023 Jul 19.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Launched

• CAS Number:

  1032900-25-6