FAK
FAK (focal adhesion kinase), also known as PTK2 protein tyrosine kinase 2 (PTK2), is a protein that, in humans, is encoded by the FAK gene. FAK is a focal adhesion-associated protein kinase involved in cellular adhesion and spreading processes. It has been shown that when FAK was blocked, breast cancer cells became less metastatic due to decreased mobility.
FAK is phosphorylated in response to integrin engagement, growth factor stimulation, and the action of mitogenic neuropeptides.Integrin receptors are heterodimeric transmembrane glycoproteins that cluster upon ECM engagement, leading to FAK phosphorylation and recruitment to focal adhesions.[13][14] FAK activity can also be attenuated by expression of its endogenous inhibitor known as FAK-related nonkinase (FRNK). Overexpression of FAK leads to inhibition of apoptosis and an increase in the prevalence of metastatic tumors.
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PF-573228是一种ATP竞争性FAK抑制剂，IC50为4 nM，作用于FAK比作用于Pyk2， CDK1/7和GSK-3β选择性约高50到250倍。
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TAE226 (NVP-TAE226)是一种有效的FAK抑制剂，IC50为5.5 nM，最有效作用于Pyk2，对InsR， IGF-1R， ALK和c-Met作用效果比其弱10到100倍左右。
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Defactinib (VS-6063, PF-04554878) 是选择性且口服具有活性的FAK激酶磷酸化抑制剂，能通过AKY依赖性通路以克服YB1介导的paclitaxel耐受，Phase 2。
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PF-562271, which is a potent ATP-competitive Pyk2/FAK dual inhibitor, has completed phase I clinical trial and is considered to be a promising drug for patients with solid tumors. PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK选择性低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
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FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor, it prevents FAK autophosphorylation at Y397 (IC50 = 1μM).
More
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PF-573228是一种ATP竞争性FAK抑制剂，IC50为4 nM，作用于FAK比作用于Pyk2， CDK1/7和GSK-3β选择性约高50到250倍。
More
-
TAE226 (NVP-TAE226)是一种有效的FAK抑制剂，IC50为5.5 nM，最有效作用于Pyk2，对InsR， IGF-1R， ALK和c-Met作用效果比其弱10到100倍左右。
More
-
Defactinib (VS-6063, PF-04554878) 是选择性且口服具有活性的FAK激酶磷酸化抑制剂，能通过AKY依赖性通路以克服YB1介导的paclitaxel耐受，Phase 2。
More
-
PF-562271, which is a potent ATP-competitive Pyk2/FAK dual inhibitor, has completed phase I clinical trial and is considered to be a promising drug for patients with solid tumors. PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK选择性低10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。
More
-
FAK Inhibitor 14 is a selective focal adhesion kinase (FAK) inhibitor, it prevents FAK autophosphorylation at Y397 (IC50 = 1μM).
More
