Target intelligence / Profile preview

KIT receptor (stem cell factor receptor) (KIT (or c-KIT, CD117))

Target
KIT (or c-KIT, CD117)
Molecular classification
Receptor tyrosine kinase (RTK), Type III receptor tyrosine kinase, Cell surface receptor
01

Overview

The KIT receptor (stem cell factor receptor, c-KIT, CD117) is a type III receptor tyrosine kinase essential for the development, proliferation, and survival of hematopoietic stem cells, mast cells, melanocytes, and germ cells[1][4][7]. It is activated by its ligand, stem cell factor (SCF), leading to receptor dimerization, autophosphorylation, and downstream signaling via PI3K/AKT, MAPK, and JAK/STAT pathways[1][4]. Aberrations in KIT, including gain-of-function mutations, drive neoplastic transformation in diseases such as gastrointestinal stromal tumors (GIST), acute myeloid leukemia (AML), mastocytosis, and other conditions[1][6][7]. Numerous small molecule inhibitors targeting the KIT tyrosine kinase domain have been developed and are clinically utilized in KIT-dependent cancers and mast cell disorders[3][6][7]. The receptor is a diagnostic and predictive biomarker in several cancers, guiding targeted therapy selection based on mutation and expression status[3][6][7].

Other names
c-KITCD117stem cell factor receptorSCFR
02

Mechanism of action

Inhibition of KIT tyrosine kinase activity, blocking downstream signaling and proliferation of KIT-expressing cells - Induction of apoptosis in malignant/mutated mast cells

03

Biological functions

Hematopoietic stem cell differentiation and proliferationMast cell development, differentiation, and survivalSignal transduction (PI3K/AKT, MAPK, JAK/STAT pathways)Cell proliferation and survival
04

Disease associations

Cancer (gastrointestinal stromal tumors, melanoma, leukemia, mastocytosis)Inflammation (mast cell-driven disorders)Other (piebaldism, male infertility, certain anemias)
05

Safety considerations

Myelosuppression (e.g., neutropenia, anemia)Nausea, vomiting, and gastrointestinal side effectsResistance via secondary KIT mutations (especially D816V)Off-target effects due to KIT expression in other tissues
06

Interacting drugs

6 more in the full profile.

07

Biomarkers

KIT (CD117) protein expression (immunohistochemistry)KIT mutational analysis (especially D816V) for patient selection (notably in GIST and mast cell neoplasms)

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