c-Kit
c-Kit (SCFR, tyrosine-protein kinase Kit,CD117) is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. c-Kit is a receptor tyrosine kinase type III, which binds to stem cell factor. When this receptor binds to stem cell factor (SCF) it forms a dimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. Signalling through c-Kit plays a role in cell survival, proliferation, and differentiation.
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BX795是TBK1和PDK1双重抑制剂，IC50分别为2 nM和6 nM，比对PKA，PKC，c-Kit和GSK3β的抑制性高50倍。
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Dovitinib是多靶点RTK抑制剂，对FLT3和c-Kit的IC50分别为1 nM和2 nM，对FGFR1/3和VEGFR1-4的IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2和Dovitinib(CHIR-258; TKI258)是多靶点RTK抑制剂，对FLT3和c-Kit的IC50分别为1 nM和2 nM，对FGFR1/3和VEGFR1-4的IC50为8-13 nM，对InsR，EGFR，c-Met，EphA2，Tie2和IGFR抑制性较弱。
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Amuvatinib (MP-470)是多靶点抑制剂，对c-Kit(D816H)，PDGFRα(V561D)和FLT3(D835Y)的IC50分别为10 nM，40 nM和81 nM。
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OSI-930是Kit，KDR和CSF-1R的抑制剂，IC50分别为80 nM，9 nM和15 nM，对Flt-1，c-Raf和Lck有接近的抑制性，但对 PDGFRα/β，Flt-3和Abl抑制性较弱。
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