Rebastinib is an orally active, non-ATP-competitive inhibitor that targets Bcr-Abl, including its wild-type and T315I mutant forms. It also demonstrates inhibitory activity against SRC, KDR, FLT3, and Tie-2, while showing minimal activity against c-Kit.
- Orally active.
- Non-ATP-competitive inhibition of Bcr-Abl.
- Effective against wild-type and T315I mutant Bcr-Abl.
- Inhibits other kinases such as SRC, KDR, FLT3, and Tie-2.
- Demonstrates low activity toward c-Kit.
- Potently inhibits both inactive and active forms of ABL1.
- Effective against several common TKI-resistant Bcr-Abl mutants.
- Inhibits proliferation of cells expressing Bcr-Abl and Ph+ cell lines.
- Reduces autophosphorylation of Bcr-Abl and phosphorylation of STAT5.