Preferred Label : FLT3/CDK4/6 Inhibitor FLX925;
NCIt definition : An orally available inhibitor of FMS-related tyrosine kinase 3 (FLT3, STK1, or FLK2)
and the cyclin-dependent kinases 4 (CDK4) and 6 (CDK6), with potential antineoplastic
activity. Upon administration, FLT3/CDK4/6 inhibitor FLX925 specifically binds to
and inhibits FLT3, which interferes with the activation of FLT3-mediated signal transduction
pathways and reduces cell proliferation in cancer cells that overexpress FLT3. In
addition FLX925 inhibits CDK4 and 6 and prevents the phosphorylation of retinoblastoma
(Rb) protein in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S
phase transition, which causes G1 phase cell cycle arrest, suppresses DNA synthesis
and inhibits cancer cell growth. FLT3, a class III tyrosine kinase receptor, is overexpressed
in a variety of cancers. Overexpression of CDK4/6, which is seen in certain types
of cancer, causes cell cycle deregulation.;
Molecule name : FLX925;
Origin ID : C120209;
UMLS CUI : C3896859;
Semantic type(s)
- concept_is_in_subset
- has_target
