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Ceritinib
$55 – $2,640
Products Details
Product 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].
Web ID
– HY-15656
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C28H36ClN5O3S
Citations
– 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 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.|Nat Cancer. 2022 Oct;3(10):1211-1227.|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.
References
– [1]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.|[2]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.|[3]Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4.|[4]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.
CAS Number
– 1032900-25-6
Molecular Weight
– 558.14
Compound Purity
– 99.98
SMILES
– CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3
Clinical Information
– Launched
Research Area
– Cancer; Endocrinology
Solubility
– DMSO : 12.5 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Anaplastic lymphoma kinase (ALK);IGF-1R;Insulin Receptor
Pathway
– Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
