Saturday, December 20, 2014

Ceritinib


Common name: Ceritinib; LDK378; LDK 378; Zykadia
Trademarks:  Zykadia
Molecular Formula: C28H36ClN5O3S
CAS Registry Number: 1032900-25-6
CAS Name: 5-Chloro-N2-[2-isopropoxy-5-methyl-4-(4-piperidinyl)phenyl]-N4-[2-(isopropylsulfonyl)phenyl]-2,4-pyrimidinediamine
Molecular Weight: 558.14
Activity: Oncolytic Drugs; Protein Kinase Inhibitor; Anaplastic Lymphoma Kinase Inhibitor; Lung Cancer Drug; ALK Inhibitor

Ceritinib synthesis: J Med Chem 2013, 56 (14), 5675-5690




References:
1. Michellys, P.-Y.; 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, 56(14), 5675–5690.
2. Chopiuk, G.; et. al. 2, 4-pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders. WO2005016894A1
3. Garcia-Echeverria, C.; et. al. 2, 4- di (phenylamino) pyrimidines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders. WO2004080980A1