PF-562271 [717907-75-0]

Catalog number: HY-10459_10mg
Brand: MedChem Express
Packing: 10 mg
Other sizes: 5 mg
10 mM
50 mg
Price: € 207.00
Expected delivery time: 10 days

Product specifications for - PF-562271 [717907-75-0]

Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 717907-75-0
Purity: >98%
Molecular Formula: C21H20F3N7O3S
Molecular weight: 507.4888
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: 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) [1] 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 uM) results in G1 arrest of PC3-M cells [1]. 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 [2]. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels [3]. 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 [1]. 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 [3].
Safety information: 
Additional information: 
Synonyms: HY-10459; PF562271; PF 562271