Orelabrutinib (ICP-022) (C007B-397984)

InformationOrelabrutinib (ICP-022) Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK) . Orelabrutinib has potential antineoplastic activity.TargetsBTKIn vitroOrelabrutinib potently inhibits BTK enzymatic activity with an IC50 value of 1.6 nM. In KINOMEscan assay conducted in parallel at 1 μM against a panel of 456 kinases, orelabrutinib only targets BTK with > 90% inhibition while ibrutinib inhibits additional many other kinases including EGFR, TEC and BMX, demonstrating orelabrutinib/'s superior kinase selectivity.In vivoOrelabrutinib has a favorable PK profile with an ideal T1/2 (~1.5-4 h) and good oral bioavailability (~20-80%) as well as prolonged BTK target occupancy in preclinical PK/PD studies. The superior selectivity translates into improved safety profile and large safety window in the GLP toxicology studies in rats and dogs.

Specifications and Purity: 10mM in DMSO

Molecular Formula: C26H25N3O3

Molecular Weight: 427.49

PubChem CID: 91667513

Isomeric SMILES: C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4