Molecular Formula: C30H31F3N8O
Molecular Weight: 576.624
Appearance: White fine powder
Bafetinib is an orally-available, ATP-competitive inhibitor of Bcr-Abl and Lyn with IC50 ethics of 11 and 26 nM, respectively. Structurally agnate to imatinib, Bafetinib possesses 10- to 50-fold greater biochemical authority as able-bodied as in corpuscle admeasurement assays (11 nM and 22 nM in K562 beef and 293T cells, respectively). In a amount of point-mutated Abl kinase domains, with the barring of T315I, Bafetinib inhibited phosphorylation abundant added potently than did imatinib.
Bafetinib inhibits the kinase action of both phosphorylated and unphosphorylated Tyr393 forms of Abl with IC50 ethics of 72 and 30 nM, respecitively. Though Bafetinib is a pGP substrate, balance concentrations are acceptable for anti-leukemic action and is added aided by analysis with cyclosporin A.
Bafetinib has been crystalline to abet corpuscle afterlife in Bcr-Abl leukemia corpuscle curve by both caspase-mediated and caspase-independent mechanisms. In vivo, this corpuscle afterlife is absolute of the action cachet of caspase.