Pazopanib, an orally available multi-kinase inhibitor of VEGFR, PDGFR, KIT, FGFR, as well as RAF, shows potent activity against a variety of solid tumors. Pazopanib是多重靶点抑制剂,对VEGFR1, VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms的IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。
MorePF-3758309, a potent ATP-competitive inhibitor of PAK1 and PAK4, displays broad anti-tumor activity in cellular proliferation and apoptosis. PF-3758309是PAK4抑制剂,IC50为1.3 nM,能抑制HCT116,A549,M24met和别的肿瘤外植体模型。
MoreDoramapimod (BIRB 796)是高度选择性p38α MAPK抑制剂,Kd为0.1 nM,对JNK2,c-RAF,Fyn,Lck,ERK-1,SYK,IKK2,ZAP-70,EGFR,HER2,PKA,PKC和PKCα/β/γ的抑制性较弱。
MoreT0070907 (T007), a potent and selective PPARγ inhibitor, can reduce α and β tubulin proteins in some cancer cell lines. T0070907是一种选择性的PPARγ抑制剂,IC50为1 nM,比作用于PPARα和PPARδ选择性高800倍以上。
MorePonatinib (AP24534)是一种新型有效的作用于Abl, PDGFRα, VEGFR2, FGFR1和Src的多靶点抑制剂, IC50分别为0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM和5.4 nM。
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