Home Angiogenesis FAK inhibitor - Apoptosis related activator PF-573228 For research use only.

PF-573228

PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.

PF-573228 Chemical Structure

PF-573228 Chemical Structure

CAS No. 869288-64-2

Purity & Quality Control

PF-573228 Related Products

Signaling Pathway

FAK Signaling Pathways

FAK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 Kinase assay ~10 μM DMSO inhibits FAK phosphorylation with IC50 of 11 nM 17395594
REF52 Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of ~100 nM 17395594
PC3 Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 100 nM 17395594
SKOV-3 Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM 17395594
L3.6p1 Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 300 nM 17395594
F-G Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 30 nM 17395594
MDCK Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 500 nM 17395594
PC3 Growth inhibitory assay 10 μM DMSO significantly inhibits cell growth. 17395594
REF52 Growth inhibitory assay 10 μM DMSO significantly inhibits cell growth. 17395594
MDCK Apoptosis assay 10 μM DMSO induces apoptosis 17395594
REF52 Apoptosis assay 10 μM DMSO induces apoptosis 17395594
REF52 Function assay 10 μM DMSO blocks serum and FN-stimulated migration 17395594
platelet Function assay 1 μM DMSO inhibits platelet aggregation and spreading 19716803
platelet Function assay 1 μM DMSO leads to inhibition of PAK and AKT 19716803
platelet Function assay 1 μM DMSO blocks calcium mobilization and dense granule secretion 19716803
4T1 Function assay DMSO abolishes the interaction between β3 integrin and TβR-II 19740433
MCF7 Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 430 nM 20354780
TamR Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 50 nM 20354780
FasR Kinase assay ~10 μM DMSO inhibits the phosphorylation of FAK Tyr397 with IC50 of 130 nM 20354780
TamR Function assay 1 μM DMSO inhibits cell migration 20354780
FasR Function assay 1 μM DMSO inhibits cell migration 20354780
endothelial cell Kinase assay 40 nM DMSO inhibits H2O2-induced phosphorylation of FAK 21212402
endothelial cell Function assay 40 nM DMSO inhibits H2O2-induced stress fiber formation 21212402
endothelial cell Apoptosis assay 40 nM DMSO inhibits apoptosis 21212402
GH3 Function assay 3 μM DMSO increases IK(Ca) amplitude 21925512
GH3 Function assay 3 μM DMSO enhances BKCa-channel activity 21925512
HUVEC cytotoxicity assay ~10 μM DMSO impairs endothelial cell viability 22075057
HUVEC Kinase assay 5 μM DMSO inhibits FAK kinase activity 22075057
HUVEC Function assay 5 μM DMSO induces cell cycle arrest 22075057
HUVEC Apoptosis assay 5 μM DMSO induces apoptosis 22075057
HUVEC Function assay 5 μM DMSO impedes endothelial cell migration and alters the cellular actin cytoskeleton 22075057
HUVEC Function assay 5 μM DMSO blocks HUVEC sprouting on collagen I gels 22075057
human peripheral blood T cells Kinase assay ~10 μM DMSO inhibits site-specific phosphorylation of FAK 23928188
human peripheral blood T cells Function assay ~10 μM DMSO impairs TCR-induced T cell morphological changes and alters activity of RhoA 23928188
human peripheral blood T cells Function assay ~10 μM DMSO inhibits phosphorylation of ZAP-70 and LAT 23928188
human peripheral blood T cells Function assay ~10 μM DMSO impairs Antigen-dependent T cell conjugation 23928188
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis.
Targets
FAK [1]
(Cell-free assay)
4 nM
In vitro
In vitro PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. [1]
Kinase Assay Affinity determination
Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3
Cell Research Cell lines REF52 or PC3 cells
Concentrations ~10 μM
Incubation Time 3 days
Method

Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted.
Experimental Result Images Methods Biomarkers Images PMID
Western blot cyclin B1 p-FAK / FAK Lamin A / Lamin C 30761269
Immunofluorescence FAK / F-actin Emerin 30761269
Growth inhibition assay Cell viability 30761269
In Vivo
In vivo Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice [2].
Animal Research Animal Models Ctrl-MT and MFCKO-MT mice
Dosages 5 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 491.49 Formula

C22H20F3N5O3S
CAS No. 869288-64-2 SDF Download PF-573228 SDF
Smiles CS(=O)(=O)C1=CC=CC(=C1)CNC2=NC(=NC=C2C(F)(F)F)NC3=CC4=C(C=C3)NC(=O)CC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 26 mg/mL ( (52.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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Frequently Asked Questions

Question 1:
Would you please let me know the detail of how to dissolve PF-573228 (Catalog No.S2013) for in vivo study (oral administration)?

Answer:
PF-573228 in 30% PEG400+0.5% Tween80+ 5% Propylene glycol at 30mg/ml is a suspension. If you will use the compound for oral gavage, this suspension is fine for it.

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