Preferred Label : TAM/c-Met Inhibitor RXDX-106;
NCIt synonyms : TYRO3/AXL/MER/c-Met Inhibitor RXDX-106; N-[4-(6,7-Dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide;
NCIt related terms : CEP-40783;
NCIt definition : An orally available and selective inhibitor of the receptor tyrosine kinase (RTK)
activity of both hepatocyte growth factor receptor (c-Met; HGFR) and receptors in
the TYRO3, AXL, and MER (TAM) family, with potential immunomodulating and antineoplastic
activities. Upon oral administration of TAM/c-Met inhibitor RXDX-106, this agent selectively
targets and binds to TYRO3, AXL, MER and c-Met, and prevents their RTK activity. This
blocks TYRO3/AXL/MER/c-Met-mediated signal transduction pathways, and inhibits the
proliferation and migration of TYRO3-, AXL-, MER- and c-Met-overexpressing tumor cells.
Inhibition of the TAM family in the tumor microenvironment (TME) activates the immune
system in the TME, reverses TAM mediated immunosuppression and enhances the anti-tumor
immune response, which lead to immune-mediated tumor cell killing. TYRO3, AXL and
MER, members of the TAM family of RTKs, are overexpressed in many tumor cell types.
TAMs play key roles in tumor cell proliferation, survival, invasion, angiogenesis
and metastasis, and their expression is associated with drug resistance and poor prognosis.
c-Met, also overexpressed in many tumor cell types, plays a critical role in tumor
formation, proliferation, invasion and metastasis, and contributes to tumor resistance.
In the TME, TAM expression on immune cells contributes to tumor cell evasion of immune
surveillance and to the negative regulation of immune responses.;
UNII : 1969ZJE05Q;
CAS number : 1437321-24-8; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1437321-24-8
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G-SRS /a ;
Molecule name : CEP-40783; RXDX 106; CEP 40783; RXDX-106;
NCI Metathesaurus CUI : CL552337;
Origin ID : C150585;
UMLS CUI : C4725852;
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- Semantic type(s)
- UMLS correspondences (same concept)
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