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- NCIT_C200317 IAO_0000115 "An orally bioavailable 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, ROS1/TRK/ALK inhibitor TY-2136b targets, binds to and inhibits ROS1, TRK, ALK alterations and resistance mutations, including acquired ROS1/TRK/ALK mutations and especially solvent front substitutions such as ROS1 G2032R/TRKA G595R/ALK G1202R mutations as well as other mutations. 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 neurotrophic tyrosine receptor kinase (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 and/or mutated in certain cancer cells, plays a key role in cell growth and survival of cancer cells. Compared to other ROS1/TRK/ALK inhibitors, TY-2136b may overcome drug resistance that is caused by acquired solvent-front mutations and may have a better ability to cross the blood-brain-barrier (BBB)." @default.
- NCIT_C200317 NCIT_A7 NCIT_C17691 @default.
- NCIT_C200317 NCIT_A7 NCIT_C27032 @default.
- NCIT_C200317 NCIT_NHC0 "C200317" @default.
- NCIT_C200317 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C200317 NCIT_P108 "ROS1/TRK/ALK Inhibitor TY-2136b" @default.
- NCIT_C200317 NCIT_P322 "GDC" @default.
- NCIT_C200317 NCIT_P399 "812628" @default.
- NCIT_C200317 normalizedInformationContent "100" @default.
- NCIT_C200317 referenceCount "1" @default.
- NCIT_C200317 hasExactSynonym "ROS1/NTRK/ALK Inhibitor TY-2136b" @default.
- NCIT_C200317 hasExactSynonym "ROS1/TRK/ALK Inhibitor TY-2136b" @default.
- NCIT_C200317 hasExactSynonym "TY 2136b" @default.
- NCIT_C200317 hasExactSynonym "TY-2136b" @default.
- NCIT_C200317 hasExactSynonym "TY2136b" @default.
- NCIT_C200317 inSubset NCIT_C128784 @default.
- NCIT_C200317 inSubset NCIT_C157711 @default.
- NCIT_C200317 inSubset NCIT_C157712 @default.
- NCIT_C200317 inSubset NCIT_C176424 @default.
- NCIT_C200317 type Class @default.
- NCIT_C200317 isDefinedBy ncit.owl @default.
- NCIT_C200317 label "ROS1/TRK/ALK Inhibitor TY-2136b" @default.
- NCIT_C200317 subClassOf NCIT_C129824 @default.
- NCIT_C200317 subClassOf NCIT_C129825 @default.
- NCIT_C200317 subClassOf NCIT_C1404 @default.
- NCIT_C200317 subClassOf NCIT_C141136 @default.
- NCIT_C200317 subClassOf NCIT_C163758 @default.
- NCIT_C200317 subClassOf NCIT_C1908 @default.
- NCIT_C200317 subClassOf NCIT_C1909 @default.
- NCIT_C200317 subClassOf NCIT_C1967 @default.
- NCIT_C200317 subClassOf NCIT_C200317 @default.
- NCIT_C200317 subClassOf NCIT_C2189 @default.
- NCIT_C200317 subClassOf NCIT_C274 @default.
- NCIT_C200317 subClassOf NCIT_C471 @default.