PF-00562271是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK抑制剂，IC50为1.5 nM，作用于Pyk2比作用于FAK效果低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。在重组酶实验中, PF-562271选择性抑制FAK 和 Pyk2 酪氨酸激酶活性，IC50分别为1.5 nM 和14 nM。在细胞实验中，PF-562271 作用于FAK的IC50值为5 nM，比作用于其他激酶靶点选择性更高。 在二维培养中，PF-562271 抑制FAK WT,FAK−/− 和FAK 激酶缺乏(KD)的细胞增殖，IC50分别为3.3 μM, 2.08 μM 和 2.01 μM。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

PF562271 besylate; PF 562271 besylate

固体粉末

DMSO ：12 mg/mL (18 mM)

FAK ,PYK2 ,CDK2/CyclinE ,CDK3/CyclinE ,CDK1/CyclinB

PF-562271 Besylate shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively.

In several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy.