Preferred Label : Rebastinib Tosylate;
NCIt synonyms : Multitargeted Tyrosine Kinase Inhibitor DCC-2036;
NCIt definition : The tosylate salt of rebastinib, an orally bioavailable small-molecule inhibitor of
multiple tyrosine kinases with potential antineoplastic activity. Rebastinib binds
to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the
folded protein to disallow ligand-dependent and ligand-independent activation; in
addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and
the receptor tyrosine kinases TIE-2 and VEGFR-2. Rebastinib may exhibit more potent
activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase
inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis,
respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety
of cellular responses including differentiation, division, adhesion, and the stress
response.;
UNII : 042A5NJE6B;
InChIKey : ARPBZBAWXAVDCE-UHFFFAOYSA-N;
CAS number : 1033893-29-6;
Molecule name : DCC-2036; DP-1919.TO;
Chemical formula : C30H28FN7O3.C7H8O3S;
ChEBI ID : CHEBI:62166;
Origin ID : C82693;
UMLS CUI : C3642434;
Semantic type(s)
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
