Preferred Label : Migoprotafib;
NCIt synonyms : SHP2 Inhibitor RLY-1971;
NCIt definition : An orally bioavailable inhibitor of protein tyrosine phosphatase (PTP) non-receptor
type 11 (SHP2; Src homology region 2 domain phosphatase; PTPN11), with potential antineoplastic
activity. Upon oral administration, migoprotafib targets, binds to and inhibits the
activity of SHP2. This prevents SHP2-mediated signaling, inhibits MAPK signaling and
prevents growth of SHP2-expressing tumor cells. SHP2, an oncoprotein overexpressed
in a variety of cancer cell types, regulates cell survival, differentiation and proliferation
through activation of the Ras-Raf-MEK-ERK signaling pathway. The Ras-MAPK pathway
is often hyperactivated in cancer cells due to specific mutations and rearrangements
and are dependent on SHP2 for their oncogenic signaling. SHP2 also regulates programmed
cell death 1 (PD-1)-mediated signal transduction and is involved in immune checkpoint
modulation.;
UNII : ABR1HZ0ZG8;
CAS number : 2377352-49-1;
Molecule name : RLY 1971; GDC 1971; RLY-1971; GDC-1971;
NCI Metathesaurus CUI : CL1906025;
Origin ID : C199073;
UMLS CUI : C5855345;
Semantic type(s)
- concept_is_in_subset
- has_target
