Art. -Nr.: HY-10461

PF-573228

39 Cited Publications

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Based on 39 publication(s) in Google Scholar

PF-573228 is a potent and selective FAK inhibitor with IC₅₀ of 4 nM for purified recombinant catalytic fragment of FAK.

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Reinheit: 99.32%
CAS. Nr.: 869288-64-2
Formel: C₂₂H₂₀F₃N₅O₃S
Molecular Weight:491.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-573228 Chemical Structure

CAS. Nr.: 869288-64-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (39)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PF-573228 is a potent and selective FAK inhibitor with IC₅₀ of 4 nM for purified recombinant catalytic fragment of FAK.

IC₅₀ & Target

IC50: 4 nM (FAK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	11 nM Compound: PF-228	Inhibition of FAK Tyr397 phosphorylation in human A431 cells by ELISA Inhibition of FAK Tyr397 phosphorylation in human A431 cells by ELISA	[PMID: 17395594]
MDCK	IC₅₀	500 nM Compound: PF-228	Inhibition of FAK Tyr397 phosphorylation in dog MDCK cells after 60 mins by Western blot analysis Inhibition of FAK Tyr397 phosphorylation in dog MDCK cells after 60 mins by Western blot analysis	[PMID: 17395594]
PC-3	IC₅₀	100 nM Compound: PF-228	Inhibition of FAK Tyr397 phosphorylation in human PC3 cells after 60 mins by Western blot analysis Inhibition of FAK Tyr397 phosphorylation in human PC3 cells after 60 mins by Western blot analysis	[PMID: 17395594]
SK-OV-3	IC₅₀	50 nM Compound: PF-228	Inhibition of FAK Tyr397 phosphorylation in human SKOV3 cells after 60 mins by Western blot analysis Inhibition of FAK Tyr397 phosphorylation in human SKOV3 cells after 60 mins by Western blot analysis	[PMID: 17395594]

In Vitro

PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC₅₀ value of 4 nM^[1].
PF-573228 inhibits FAK phosphorylation on Tyr₃₉₇ with an IC₅₀ value of 30-100 nM^[1].
PF-573228 significantly decreased FAK Tyr₃₉₇ phosphorylation^[1].
PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 869288-64-2
Appearance Solid
Molecular Weight 491.49
Formel C₂₂H₂₀F₃N₅O₃S
Color White to off-white
SMILES

O=C1NC2=C(C=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC(S(=O)(C)=O)=C4)=N3)C=C2)CC1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (39)

All WBIF

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Journal Impact Factor

Signal Transduct Target Ther

p53 positively regulates the proliferation of hepatic progenitor cells promoted by laminin-521. [Abstract]

2022 Aug 31;7(1):290. PMID: 36042225
Nat Nanotechnol

Nanoparticles reach metastatic tumours via enhanced permeability of adjacent vessels. [Abstract]

2026 Jun;21(6):880-891. PMID: 42286217
Adv Mater

Engineered Perfusable Hepatic Fibrosis Model via Embedded Sacrificial Bioprinting Recapitulates Stiffness-Driven Fibrogenesis. [Abstract]

2026 Mar;38(13):e13401. PMID: 41568614
Bone Res

Endothelial PDGF-BB/PDGFR-β signaling promotes osteoarthritis by enhancing angiogenesis-dependent abnormal subchondral bone formation. [Abstract]

2022 Aug 29;10(1):58. PMID: 36031625
Autophagy

PTK2/FAK inhibition triggers TMED9-mediated protective autophagy in pancreatic cancer cell via enhancing ERGIC-ERES contact. [Abstract]

2026 May 29:1-15. PMID: 42144738
Nat Commun

The integrin repertoire drives YAP-dependent epithelial:stromal interactions during injury of the kidney glomerulus. [Abstract]

2025 Apr 8;16(1):3322. PMID: 40199893
Cell Discov

Cancer cells sense solid stress to enhance metastasis by CKAP4 phase separation-mediated microtubule branching. [Abstract]

2024 Nov 12;10(1):114. PMID: 39528501
Adv Sci (Weinh)

Heterogeneous Responses to Mechanical Force of Prostate Cancer Cells Inducing Different Metastasis Patterns. [Abstract]

2020 Jun 17;7(15):1903583. PMID: 32775149

PF-573228 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583. [Abstract]

Fluorescence imaging of LNCaP cells treated with the F-actin inhibitor cytoskeleton B (CB), microtubule inhibitor nocodazole (NO), FAK inhibitor PF573288 (PF), ROCK inhibitor Y-27632 (Y), and myosin II (Myo-II) inhibitor (-)-blebbistatin ((-)Bl). After the cells were cultured on different substrates for 3 days, inhibitors were added and incubated for 24 h. (green, F-actin; scale bar, 25 µm).

PF-573228 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583. [Abstract]

Expression of CTC cluster-related (plakoglobin and CD44) and EMT-related (vimentin and E-cadherin, 4 days) proteins in LNCaP cells grown on different substrates after treatment with different inhibitors (Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl)).
Sci Adv

Diabetic hyperglycemia promotes primary tumor progression through glycation-induced tumor extracellular matrix stiffening. [Abstract]

2022 Nov 16;8(46):eabo1673. PMID: 36399580
Biomaterials

FAK-p38 signaling serves as a potential target for reverting matrix stiffness-modulated liver sinusoidal endothelial cell defenestration. [Abstract]

2024 Mar:305:122462. PMID: 38171118
Biomaterials

Untangling the response of bone tumor cells and bone forming cells to matrix stiffness and adhesion ligand density by means of hydrogels. [Abstract]

2019 Jan:188:130-143. PMID: 30343256
Biomaterials

Mechanically cartilage-mimicking poly(PCL-PTHF urethane)/collagen nanofibers induce chondrogenesis by blocking NF-kappa B signaling pathway. [Abstract]

2018 Sep:178:281-292. PMID: 29945065
Cell Death Dis

Septin11 promotes hepatocellular carcinoma cell motility by activating RhoA to regulate cytoskeleton and cell adhesion. [Abstract]

2023 Apr 20;14(4):280. PMID: 37080972
Acta Pharmacol Sin

Resibufogenin promotes angiogenesis via the VAV3-mediated ITGA5-VEGF signaling axis in macrophages to alleviate myocardial infarction. [Abstract]

2026 Apr 29. PMID: 42056214
Acta Pharmacol Sin

Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. [Abstract]

2023 May;44(5):984-998. PMID: 36450791
Dev Cell

STAT3-controlled CHI3L1/SPP1 positive feedback loop demonstrates the spatial heterogeneity and immune characteristics of glioblastoma. [Abstract]

2025 Jun 23;60(12):1751-1767.e9. PMID: 39933531
Int J Biol Macromol

Dual scalable osteogenic microtissue engineering via GelMA microsphere-inspired mechanical training and autonomous assembling of dental pulp stem cell. [Abstract]

2024 Dec;282(Pt 1):136258. PMID: 39395512
Int J Biol Macromol

Adipocyte-secreted PRELP promotes adipocyte differentiation and adipose tissue fibrosis by binding with p75NTR to activate FAK/MAPK signaling. [Abstract]

2024 Nov;279(Pt 4):135376. PMID: 39244119
Antioxidants (Basel)

Effect of Extracellular Matrix Stiffness on Candesartan Efficacy in Anti-Fibrosis and Antioxidation. [Abstract]

2023 Mar 9;12(3):679. PMID: 36978927
Cell Rep

Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells. [Abstract]

2023 May 17;42(5):112529. PMID: 37200193
J Invest Dermatol

FAK-Dependent Reprogramming of IFN-γ Signaling through PYK2 Co-Inhibition Sensitizes Melanoma to Immune Checkpoint Blockade. [Abstract]

2025 Oct 14:S0022-202X(25)03407-4. PMID: 41101630
J Cell Biol

MYO18B promotes lysosomal exocytosis by facilitating focal adhesion maturation. [Abstract]

2025 Mar 3;224(3):e202407068. PMID: 39751400
Commun Biol

TGFBI promotes liver fibrosis through remodeling the profibrotic microenvironment by a positive feedback regulatory loop. [Abstract]

2026 Feb 3;9(1):355. PMID: 41634371
Cancer Biol Ther

Netrin-1 inducing antiapoptotic effect of acute myeloid leukemia cells in a concentration-dependent manner through the Unc-5 netrin receptor B-focal adhesion kinase axis. [Abstract]

2023 Dec 31;24(1):2200705. PMID: 37038247
Pharmaceuticals (Basel)

Potential Antimetastatic Effect of Timosaponin AIII against Human Osteosarcoma Cells through Regulating the Integrin/FAK/Cofilin Axis. [Abstract]

2021 Mar 14;14(3):260. PMID: 33799345
Int Immunopharmacol

Osteopontin induces airway smooth muscle cells proliferation and migration by modulating FAK/Src/YAP axis. [Abstract]

2026 Jan 15:169:115886. PMID: 41349465
Int Immunopharmacol

SPP1 as a key modulator of M2 macrophage polarization promotes endometriosis progression via activation of the FAK/PI3K/AKT pathway: A bioinformatics and experimental study. [Abstract]

2025 Sep 17:166:115563. PMID: 40967048
J Pathol

Periostin deficiency reduces diethylnitrosamine-induced liver cancer in mice by decreasing hepatic stellate cell activation and cancer cell proliferation. [Abstract]

2021 Oct;255(2):212-223. PMID: 34228359
Mol Nutr Food Res

High-Fat-Diet-Induced Extracellular Matrix Deposition Regulates Integrin-FAK Signals in Adipose Tissue to Promote Obesity. [Abstract]

2022 Apr;66(7):e2101088. PMID: 35106921
FASEB J

Selective depletion of hepatic stellate cells-specific LOXL1 alleviates liver fibrosis. [Abstract]

2021 Oct;35(10):e21918. PMID: 34569648
Cell Adh Migr

Fibronectin induces macrophage migration through a SFK-FAK/CSF-1R pathway. [Abstract]

2017 Jul 4;11(4):327-337. PMID: 27588738

PF-573228 purchased from MedChemExpress. Usage Cited in: Cell Adh Migr. 2017 Jul 4;11(4):327-337. [Abstract]

BAC1.2F5 cells are cultured in the absence of CSF-1 for 18 hours and then kept in suspension for 45 minutes and lysed (0) or plated on FN-coated dishes (10 mg/mL) for 30 minutes in the presence or the absence of PF-573228 (1 mM) before lysis. Proteins are subjected to immunoblotting with the indicated antibodies.
Am J Physiol Heart Circ Physiol

Exercise training ameliorates myocardial dysfunction through fibronectin-mediated mechanotransduction in a swine model of ischemic heart disease. [Abstract]

2026 Jan 1;330(1):H31-H45. PMID: 41247790
Biochem Biophys Rep

Exosome-mediated transduction of mechanical force regulates prostate cancer migration via microRNA. [Abstract]

2022 Jul 2:31:101299. PMID: 35812347
BMC Neurol

Integrated analysis of bulk and single-cell RNA sequencing reveals the impact of nicotinamide and tryptophan metabolism on glioma prognosis and immunotherapy sensitivity. [Abstract]

2024 Oct 28;24(1):419. PMID: 39468708
FASEB Bioadv

Levo-Tryptophan Promotes Osteogenesis Through Calcium-Sensing Receptor. [Abstract]

2025 Sep 3;7(8):e70045. PMID: 40909871
Rapid Commun Mass Spectrom

Chishizhi Yuyuliang Decoction Ameliorates Ulcerative Colitis in Mice by Promoting Colonic Epithelial Mucosal Healing via the CAV1/FA Axis. [Abstract]

2026 Aug 30;40(16):e70106. PMID: 42200545
Jundishapur J Microbiol

2025 Apr 6;18(5):e160281.
bioRxiv

Circulating biomarkers in serum from aortic valve stenosis patients predict sex-specific drug responses in valve myofibroblasts. [Abstract]

2026 Jan 20:2026.01.16.700010. PMID: 41648356
bioRxiv

Convergent flow-mediated mesenchymal force drives embryonic foregut constriction and splitting. [Abstract]

2025 Jan 23:2025.01.22.634318. PMID: 39896544

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (50.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0346 mL

10.1731 mL

20.3463 mL

5 mM

0.4069 mL

2.0346 mL

4.0693 mL

10 mM

0.2035 mL

1.0173 mL

2.0346 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Purified activated FAK kinase domain 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 for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with s

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

REF52 or PC3 cells are seeded into a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor (PF-573228) for 3 days. Subsequently, the cells are harvested and counted. Apoptosis assays are performed using a cell death detection ELISA. REF52, PC3 or MDCKcells are treated for 24 h (16 h for MDCK) with the indicated concentrations of each inhibitor prior to lysis. Cells suspended for 16-24 h in serum-free medium served as a positive control. The cell lysates are incubated in duplicate in the ELISA system. The data represent the means±standard deviation of one of three experiments performed in duplicate^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0346 mL	10.1731 mL	20.3463 mL	50.8657 mL
	5 mM	0.4069 mL	2.0346 mL	4.0693 mL	10.1731 mL
	10 mM	0.2035 mL	1.0173 mL	2.0346 mL	5.0866 mL
	15 mM	0.1356 mL	0.6782 mL	1.3564 mL	3.3910 mL
	20 mM	0.1017 mL	0.5087 mL	1.0173 mL	2.5433 mL
	25 mM	0.0814 mL	0.4069 mL	0.8139 mL	2.0346 mL
	30 mM	0.0678 mL	0.3391 mL	0.6782 mL	1.6955 mL
	40 mM	0.0509 mL	0.2543 mL	0.5087 mL	1.2716 mL
	50 mM	0.0407 mL	0.2035 mL	0.4069 mL	1.0173 mL

Keywords

PF-573228

39 Cited Publications

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PF-573228

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-573228

Biologische Aktivität

Chemical Information

Publications (39)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-573228

Cytoskeleton Compound Library

Anti-Pancreatic Cancer Compound Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-573228

Biologische Aktivität

Chemical Information

Publications (39)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-573228 Related Classifications

HY-10461 Related Classifications