PF-00562271

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-00562271 是 PF-562271 的苯磺酸盐，PF-562271 是一种有效的 ATP 竞争性、可逆的 FAK 抑制剂，IC50 为 1.5 nM。

PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1.(In Vitro):PF-562271 (VS-6062) besylate 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.

PF-562271 (VS-6062) besylate 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.

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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Angiogenesis

CDK

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

Cancer

Solid Tumors

939791-38-5

665.66

C21H20F3N7O3S.C6H6O3S

>98% (HPLC)

DMSO:14 mg/mL warmed (21.03 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)

OS(=O)(=O)C1=CC=CC=C1.CN(C1=C(CNC2=C(C=NC(NC3=CC=C4NC(=O)CC4=C3)=N2)C(F)(F)F)C=CC=N1)S(C)(=O)=O |c:6,8,12,18,31,33,40,42,t:4,16,22,24|

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(-20℃)

With Ice Pack

≥ 2 years