Ceritinib dihydrochloride
Product Specifications
UNSPSC Description
Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) 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-dihydrochloride.html
Solubility
DMSO : 100 mg/mL (ultrasonic)|H2O : 10 mg/mL (ultrasonic)
Smiles
CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.[H]Cl.[H]Cl
Molecular Weight
631.06
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, Jun 6.|[2]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.bioRxiv. 2023 Jul 19.|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.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-15656A/Ceritinib-dihydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-15656A/Ceritinib-dihydrochloride-SDS-MedChemExpress.pdf
Clinical Information
Launched
CAS Number
1380575-43-8
Available Sizes
Curated Selection
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