Home Angiogenesis FAK inhibitor - Pyk2 inhibitor - CDK inhibitor PF-562271 HCl For research use only.

PF-562271 HCl

PF-562271 HCl is the hydrochloride 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.

PF-562271 HCl Chemical Structure

PF-562271 HCl Chemical Structure

CAS No. 939791-41-0

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PF-562271 HCl Related Products

Signaling Pathway

FAK Signaling Pathways

FAK Signaling Pathway

Biological Activity

Description PF-562271 HCl is the hydrochloride 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.
Features Dual FAK/Pyk2 inhibitor that has been tested in Phase I clinical trials for treatment of pancreatic, head and neck, and prostate cancers.
Targets
FAK [1] PYK2 [1] CDK2/CyclinE [1] CDK3/CyclinE [1] CDK1/CyclinB [1] Click to View More Targets
1.5 nM 13 nM 30 nM 47 nM 58 nM
In vitro
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. [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
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] PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. [4] 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. [5]
Animal Research Animal Models Athymic female mice bearing BxPc3 or PC3-M xenografts.
Dosages 50 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 543.95 Formula

C21H21ClF3N7O3S
CAS No. 939791-41-0 SDF Download PF-562271 HCl SDF
Smiles CN(C1=C(C=CC=N1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)C4)S(=O)(=O)C.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (183.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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