PF-562271 HCl

PF-562271 是一种强效的、ATP竞争性的和可逆的局部粘着斑激酶(FAK)和富含脯氨酸的酪氨酸激酶2 (Pyk2)抑制剂，半数最大抑制浓度（IC50）分别为1.5 nmol/L和14 nmol/L。FAK是一种参与多种细胞活动的非受体酪氨酸激酶，而Pyk2是一种含有48% 氨基酸同源性的FAK 同系物。据报道，作为用于癌症治疗的一种潜在的治疗剂，无论单一用药或是与其他治疗剂联合用药，PF-562271在异种移植和转基因小鼠模型中都有效抑制肿瘤的扩散，其中在带有肿瘤的小鼠中剂量依赖性地抑制FAK 磷酸化，半数最大有效浓度(EC50)为93 ng/mL。

参考文献：
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