Src
There are 9 members part of the Src family kinases: c-Src , Yes, Fyn, Fgr, Yrk, Lyn, Blk, Hck, and Lck.[8] The expression of these Src family members are not the same throughout all tissues and cell types. Src, Fyn and Yes are expressed ubiquitously in all cell types while the others are generally found in hematopoietic cells. When src is activated, it promotes survival, angiogenesis, proliferation and invasion pathways. It also regulates angiogenic factors and vascular permeability after focal cerebral ischemia-reperfusion,[16][17] and regulates matrix metalloproteinase-9 activity after intracerebral hemorrhage.
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Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂,其IC50分别为1.2 nM和1 nM。
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PP1
EY1619
PP1(AGL 1872)是Src选择性抑制剂,对Lck和Fyn的IC50分别为5 nM和6 nM。
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PP2
EY1272
PP2是一种Src家族激酶抑制剂,有效抑制Lck/Fyn,IC50为4 nM/5 nM,作用于EGFR效果低100倍左右,同时抑制ZAP-70, JAK2和PKA的活性。
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Saracatinib (AZD0530)是一种有效的Src抑制剂,IC50为2.7 nM,对c-Yes, Fyn, Lyn, Blk, Fgr和Lck等也有活性;但对Abl和EGFR (L858R和L861Q)活性较低。
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WH-4-023是一种强效且口服有效的Lck/Src抑制剂,其IC50分别为2nM and 6 nM。
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