cerdulatinib   Click here for help

GtoPdb Ligand ID: 8957

Synonyms: PRT 062070 | PRT-062070 | PRT-2070 | PRT062070
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Cerdulatinib (PRT062070) is an investigational kinase inhibitor, with dual activity against Janus kinases (JAKs) and spleen tyrosine kinase (SYK) pathways [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 10
Hydrogen bond donors 3
Rotatable bonds 8
Topological polar surface area 141.93
Molecular weight 445.19
XLogP 1.83
No. Lipinski's rules broken 0
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Canonical SMILES CCS(=O)(=O)N1CCN(CC1)c1ccc(cc1)Nc1ncc(c(n1)NC1CC1)C(=O)N
Isomeric SMILES CCS(=O)(=O)N1CCN(CC1)c1ccc(cc1)Nc1ncc(c(n1)NC1CC1)C(=O)N
InChI InChI=1S/C20H27N7O3S/c1-2-31(29,30)27-11-9-26(10-12-27)16-7-5-15(6-8-16)24-20-22-13-17(18(21)28)19(25-20)23-14-3-4-14/h5-8,13-14H,2-4,9-12H2,1H3,(H2,21,28)(H2,22,23,24,25)
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Summary of Clinical Use Click here for help
Cerdulatinib is being evaluated in Phase 1 clinical trial for its potential to treat chronic lymphocytic leukaemia (CLL) and lymphomas (small lymphocytic lymphoma, SLL and non-Hodgkin lymphoma, NHL)- see clinical trial NCT01994382.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Cerdulatinib is a reversible ATP-competitive small molecule kinase inhibitor. SYK and JAK independently contribute to the pathogenesis of certain autoimmune and malignant disorders, therefore simultaneous inhibition of both pathways is expected to deliver improved disease therapy in comparision to selective kinase inhibition.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT01994382 Phase 1/2A Dose Escalation Study in CLL, SLL or NHL Phase 1/Phase 2 Interventional Portola Pharmaceuticals