Ceritinib

• 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].

• Product Name Alternative :

  LDK378

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H320, H335

• Target :

  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

• Purity :

  99.95

• 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 Formula :

  C28H36ClN5O3S

• Molecular Weight :

  558.14

• Precautions :

  H302, H315, H320, H335

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Citation 01 :

  AMB Express. 2022 Nov 28;12 (1) :150.|Analyst. 2025 Dec 1;150 (24) :5501-5513.|Anim Reprod Sci. 2025 Apr 28:277:107850.|Biochim Biophys Acta Mol Cell Res. 2020 Jul;1867 (7) :118712.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biol Methods Protoc. 2025 Feb 13;10 (1) :bpaf012.|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 Feb 21;4 (2) :100911.|Cell Rep Med. 2025 Apr 2:102053.|Cell Signal. 2022 Apr:92:110264.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Eur J Med Chem. 2023 Jan 15:246:114946.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|Harvard Medical School LINCS LIBRARY|J Med Chem. 2024 Oct 24;67 (20) :18098-18123.|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. 2024 Jan;20 (1) :28-55.|Nat Cancer. 2022 Oct;3 (10) :1211-1227.|Nat Commun. 2024 Apr 23;15 (1) :3422.|Patent. US20200276189A1.|Patent. US20230158019A1.|Pharmaceuticals (Basel) . 2024 Feb 2;17 (2) :197.|Pharmacol Res. 2025 Nov:221:107993.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|PLoS One. 2025 Jan 21;20 (1) :e0308747.|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.|Toxicol Appl Pharmacol. 2025 Oct:503:117489.|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.|Nat Commun. 2025 Aug 23;16 (1) :7870.

• CAS Number :

  [1032900-25-6]