FLT3
FLT3 (fms like tyrosine kinase 3,Cluster of differentiation antigen 135 (CD135) ,fetal liver kinase-2 (Flk2)) is a protein that is a cytokine receptor which belongs to the receptor tyrosine kinase class III. FLT3 is the receptor for the cytokine Flt3 ligand (FLT3L). It is expressed on the surface of many hematopoietic progenitor cells. Signalling of FLT3 is important for the normal development of haematopoietic stem cells and progenitor cells. Signaling through FLT3 plays a role in cell survival, proliferation, and differentiation.
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Dovitinib (TKI-258) Dilactic Acid 是一种多靶点的RTK抑制剂,作用于III型(FLT3/c-Kit)最有效,IC50为1 nM/2 nM,也有效作用于IV型(FGFR1/3)和V型(VEGFR1-4)RTKs,IC50为8-13 nM,对InsR, EGFR, c-Met, EphA2, Tie2, IGFR1和HER2作用效果稍弱。
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ENMD-2076是Aurora A和Flt3抑制剂,IC50分别为14 nM和1.86 nM,比对 Aurora B的抑制性高25倍,对VEGFR2/KDR,VEGFR3,FGFR1,FGFR2和PDGFRα的抑制性较弱。
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TG101209是JAK2选择性抑制剂,IC50为6 nM,对Flt3和RET的IC50为25 nM和17 nM,比对JAK3的抑制性高30倍,对JAK2V617F和MPLW515L/K突变型敏感,还能抑制BRD4,IC50为130 nM。
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