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Products are for research use only. Not for human use. We do not sell to patients.
(PF562271; PF 562271)
PF-562271 Chemical Structure
|Product name: PF-562271|
|Cat. No.: HY-10459|
PF-562271 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.
IC50 value: 1.5 nM(FAK); 14 nM(Pyk2) 
Target: PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells . PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage . PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels .
in vivo: PF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts . PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement .
|M.Wt||507.49||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 48 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.9705 mL||9.8524 mL||19.7048 mL|
|5 mM||0.3941 mL||1.9705 mL||3.9410 mL|
|10 mM||0.1970 mL||0.9852 mL||1.9705 mL|
. Canel M, et al. Quantitative in vivo imaging of the effects of inhibiting integrin signaling via Src and FAK on cancer cell movement: effects on E-cadherin dynamics. Cancer Res, 2010, 70(22), 9413-9422.
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