NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

FLT3 inhibitor SKI-G-801
An orally bioavailable inhibitor of both wild type and mutant forms of FMS-like tyrosine kinase 3 (FLT3; CD135; STK1; FLK2), with potential antineoplastic activity. Upon administration, FLT3 inhibitor SKI-G-801 binds to and inhibits the activity of FLT3, including FLT3-ITD (internal tandem duplications), FLT3-D835Y as well as other mutants. This inhibits uncontrolled FLT3 signaling and results in the inhibition of proliferation in tumor cells overexpressing FLT3. FLT3, a class III receptor tyrosine kinase (RTK), is overexpressed or mutated in most B lineage neoplasms and in acute myeloid leukemias, and plays a key role in tumor cell proliferation. In addition, SKI-G-801 also inhibits, to a lesser degree, the receptor tyrosine kinases AXL (UFO), Mer, Ret, vascular endothelial growth factor receptor 1 (VEGFR1), Fms, fibroblast growth factor receptors (FGFR) 1 and 3, and the serine/threonine kinases Aurora B and C. Check for active clinical trials using this agent. (NCI Thesaurus)

Synonym:FLT3 kinase inhibitor SKI-G-801
FLT3 tyrosine kinase inhibitor SKI-G-801
G-749 HCl salt
G749 hydrochloride
Code name:G-801