2055376-74-2
2055376-74-2
Chemical Structure
Ceritinib mesylate
Synonym(s): LDK378 mesylate
- CAS No.: 2055376-74-2
- Formula:C30H44ClN5O9S3
- Molecular Weight:750.35
InChIKey: WTRLZBZDHQPJDE-UHFFFAOYSA-N
SMILES: CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3.CS(=O)(O)=O.CS(=O)(O)=O
Biological Activity: Ceritinib (LDK378) mesylate is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib mesylate shows great antitumor potency[1][2].
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Ceritinib mesylate | Ceritinib (LDK378) mesylate is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib mesylate also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib mesylate shows great antitumor potency. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [Content Brief]
