Preferred Label : pan-RAF Inhibitor XP-102;
NCIt synonyms : 1-Propanesulfonamide, N-(3-(5-((1-ethyl-4-piperidinyl)methylamino)-3-(5-pyrimidinyl)-1H-pyrrolo(3,2-b)pyridin-1-yl)-2,4-difluorophenyl)-; N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide;
NCIt related terms : XP-102;
NCIt definition : An orally bioavailable, second-generation inhibitor of all members of the serine/threonine
protein kinase Raf family, including A-Raf, B-Raf and C-Raf protein kinases, with
potential antineoplastic activity. Upon administration, pan-RAF kinase inhibitor XP-102
specifically binds to the ATP binding site of the Raf kinase positioned in the inactive
DFG-out conformation, and inhibits the activity of Raf, including B-Raf mutated forms
such as the B-Raf V600E mutation. This prevents the activation of Raf-mediated signal
transduction pathways, which may inhibit tumor cell growth. Raf protein kinases play
a key role in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular
signal-regulated kinase (ERK) signaling pathway, which is often dysregulated in human
cancers and plays a key role in tumor cell proliferation and survival. The valine
to glutamic acid substitution at residue 600 accounts for the majority of BRAF gene
mutations. The oncogenic product, BRAF(V600E) kinase, exhibits elevated activity that
over-activates the MAPK signaling pathway.;
UNII : V32TR55QP9;
CAS number : 1392429-79-6;
Molecule name : XP-102; BI-882370; XP 102; BI 882370;
NCI Metathesaurus CUI : CL1792007;
Origin ID : C187123;
UMLS CUI : C5706370;
Semantic type(s)
- concept_is_in_subset
- has_target
