PF-562271 - Moligand™, 10mM in DMSO , Inhibitor of aurora kinase A;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta, CAS No.717907-75-0, Inhibitor of aurora kinase A;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
PF-562271 - Moligand™, 10mM in DMSO , Inhibitor of aurora kinase A;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta, CAS No.717907-75-0, Inhibitor of aurora kinase A;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Descripción general
Information
PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor ofFAKwithIC50of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for someCDKs. In vitro
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. PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia. Cell Data
PF-562271 (PF-00562271) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
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Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Inhibitor of aurora kinase A;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of protein tyrosine kinase 2;Inhibitor of protein tyrosine kinase 2 beta
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