Technology Bundle ID
TAB-3504

Discovery of imidazo[1,2-a]pyrazines with Anticancer Properties

Applications
Linked ID
E-047-2021-0
Lead Inventors
Craig Thomas (NCATS)
Co-Inventors
Daniel Starczynowski (Cincinnati Children's Hospital Medical Center)
Scott Hoyt (NCATS)
ICs
This technology includes a series of imidazo[1,2-a]pyrazines that display potent inhibition of FLT3, as well as potent binding and activity against FLT3 tyrosine kinase domain and gatekeeper mutations. This chemotype exhibits superior anti-leukemic activity against the common clinically-relevant FLT3-mutant acute myeloid leukemia (AML) in vitro and in vivo. Tyrosine kinase domain mutations are a common cause of acquired resistance to FLT3 inhibitors used to treat FLT3-mutant AML.
Commercial Applications
If successful in human clinical trials, these agents could be used to treat a variety of hematological diseases, including but not limited to AML, myelodysplastic syndrome, diffuse large B-cell lymphoma, and other blood cancers.
Competitive Advantages
These agents have activity versus mutations in the acquired resistance space and versus non-IRAK inhibitors in the adaptive resistance space.

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