Rebastinib (DCC-2036) is an orally active, non-ATP-competitive inhibitor targeting Bcr-Abl, including resistant mutants. It effectively inhibits Abl1WT and Abl1T315I, as well as SRC, KDR, FLT3, and Tie-2, with low activity against c-Kit. This compound demonstrates potent antiproliferative effects in various leukemia cell lines and significantly prolongs survival in animal models of leukemia.
- Potently inhibits ABL1 native and ABL1 T315I.
- Inhibits SRC family kinases and PDGFRα/β.
- Selectively spares c-KIT.
- Effectively inhibits proliferation of native BCR-ABL1 and Ph+ K562 cell lines.
- Inhibits proliferation of common TKI-resistant BCR-ABL1 mutants.
- Reduces leukemia cell burden in treated mice.