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Version: 17.06d (Release date: 2017-06-26)
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Rebastinib Tosylate (Code C82693)

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Terms & Properties

Preferred Name: Rebastinib Tosylate

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.

Display Name: Rebastinib Tosylate

Label: Rebastinib Tosylate

NCI Thesaurus Code: C82693 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2830217  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
DCC-2036
DP-1919.TO
Rebastinib Tosylate

External Source Codes: 
CAS Registry Number 1033893-29-6 (see NLM ChemIDplus info)
ChEBI ID CHEBI:62166 (see ChEBI info)
PDQ Closed Trial Search ID 634547
PDQ Open Trial Search ID 634547 (check for NCI PDQ open clinical trial info)
UMLS CUI C2830217

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C30H28FN7O3.C7H8O3S
code C82693
Contributing_Source CTRP
Legacy_Concept_Name Multitargeted_Tyrosine_Kinase_Inhibitor_DCC-2036
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C82693

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