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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KX2-391 (KX-01), the first peptidomimetic Src kinase inhibitor, is a synthetic, orally bioavailable inhibitor that has tubulin polymerization inhibition as a second mechanism of action, and is currently in Phase-2 testing for solid tumors. KX2-391 (KX01)是第一个进入临床的拟肽类Src抑制剂,靶向Src的多肽底物结合位点,对多种癌细胞株GI50为9-60 nM。
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SU 6656是Src激酶家族抑制剂,对Src、Yes、Lyn和Fyn的IC50值分别为280、20、130和170nM。
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