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PF-562271 besylate

CAS No. : 939791-38-5

MCE 站：PF-562271 besylate

产品活性：PF-562271 besylate 是有效，可逆，ATP竞争性的 FAK 和 Pyk2 激酶抑制剂，IC₅₀ 分别为 1.5 和 13 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FAK  |  Pyk2

In Vitro: PF-562,271 is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength.

In Vivo: PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC₅₀ of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo.

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