Preferred Label : TRK/ROS1/ALK Inhibitor SIM1803-1A;
NCIt definition : An orally available inhibitor of multiple kinases, including the receptor tyrosine
kinase anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), and the tropomyosin-related-kinase
(tyrosine receptor kinase; TRK), with potential antineoplastic activity. Upon oral
administration, TRK/ROS1/ALK inhibitor SIM1803-1A targets, binds to and inhibits wild-type,
point mutants and fusion proteins of ALK, ROS1, and TRK, including fusion proteins
containing sequences from neurotrophic tyrosine receptor kinase (NTRK) types 1 (NTRK1;
TrkA), 2 (NTRK2; TrkB), and 3 (NTRK3; TrkC). Inhibition of these kinases leads to
the disruption of downstream signaling pathways and the inhibition of cell growth
of tumors in which these kinases are overexpressed, rearranged or mutated. TRK, a
family of receptor tyrosine kinases (RTKs) activated by neurotrophins, is encoded
by NTRK family genes. The expression of either mutated forms of, or fusion proteins
involving, NTRK family members results in uncontrolled TRK signaling, which plays
an important role in tumor cell growth, survival, invasion and treatment resistance.
ALK belongs to the insulin receptor superfamily and plays an important role in nervous
system development; ALK dysregulation and gene rearrangements are associated with
a series of tumors. ROS1, overexpressed in certain cancer cells, plays a key role
in cell growth and survival of cancer cells.;
Molecule name : SIM1803-1A; SIM1803 1A;
NCI Metathesaurus CUI : CL1662160;
Origin ID : C179616;
UMLS CUI : C5555817;
Semantic type(s)
- concept_is_in_subset
- has_target
