PF-573228
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.
For research use only. We do not sell to patients.
- Purity: 99.32%
- CAS No.: 869288-64-2
- Formula: C22H20F3N5O3S
- Molecular Weight:491.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) PF-573228
More- Signal Transduct Target Ther. 2022 Aug 31;7(1):290. [Abstract]
- Nat Nanotechnol. 2026 Jun;21(6):880-891. [Abstract]
- Adv Mater. 2026 Mar;38(13):e13401. [Abstract]
- Bone Res. 2022 Aug 29;10(1):58. [Abstract]
- Autophagy. 2026 May 29:1-15. [Abstract]
- Nat Commun. 2025 Apr 8;16(1):3322. [Abstract]
- Cell Discov. 2024 Nov 12;10(1):114. [Abstract]
- Adv Sci (Weinh). 2020 Jun 17;7(15):1903583. [Abstract]
- Sci Adv. 2022 Nov 16;8(46):eabo1673. [Abstract]
- Biomaterials. 2024 Mar:305:122462. [Abstract]
- Biomaterials. 2019 Jan:188:130-143. [Abstract]
- Biomaterials. 2018 Sep:178:281-292. [Abstract]
- Cell Death Dis. 2023 Apr 20;14(4):280. [Abstract]
- Acta Pharmacol Sin. 2026 Apr 29. [Abstract]
- Acta Pharmacol Sin. 2023 May;44(5):984-998. [Abstract]
- Dev Cell. 2025 Jun 23;60(12):1751-1767.e9. [Abstract]
- Int J Biol Macromol. 2024 Dec;282(Pt 1):136258. [Abstract]
- Int J Biol Macromol. 2024 Nov;279(Pt 4):135376. [Abstract]
- Antioxidants (Basel). 2023 Mar 9;12(3):679. [Abstract]
- Cell Rep. 2023 May 17;42(5):112529. [Abstract]
- J Invest Dermatol. 2025 Oct 14:S0022-202X(25)03407-4. [Abstract]
- J Cell Biol. 2025 Mar 3;224(3):e202407068. [Abstract]
- Commun Biol. 2026 Feb 3;9(1):355. [Abstract]
- Cancer Biol Ther. 2023 Dec 31;24(1):2200705. [Abstract]
- Pharmaceuticals (Basel). 2021 Mar 14;14(3):260. [Abstract]
- Int Immunopharmacol. 2026 Jan 15:169:115886. [Abstract]
- Int Immunopharmacol. 2025 Sep 17:166:115563. [Abstract]
- J Pathol. 2021 Oct;255(2):212-223. [Abstract]
- Mol Nutr Food Res. 2022 Apr;66(7):e2101088. [Abstract]
- FASEB J. 2021 Oct;35(10):e21918. [Abstract]
- Cell Adh Migr. 2017 Jul 4;11(4):327-337. [Abstract]
- Am J Physiol Heart Circ Physiol. 2026 Jan 1;330(1):H31-H45. [Abstract]
- Biochem Biophys Rep. 2022 Jul 2:31:101299. [Abstract]
- BMC Neurol. 2024 Oct 28;24(1):419. [Abstract]
- FASEB Bioadv. 2025 Sep 3;7(8):e70045. [Abstract]
- Rapid Commun Mass Spectrom. 2026 Aug 30;40(16):e70106. [Abstract]
- Jundishapur J Microbiol. 2025 Apr 6;18(5):e160281.
- bioRxiv. 2026 Jan 20:2026.01.16.700010. [Abstract]
- bioRxiv. 2025 Jan 23:2025.01.22.634318. [Abstract]
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IF
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WB
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WB
Biological Activity
IC50: 4 nM (FAK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
11 nM
Compound: PF-228
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Inhibition of FAK Tyr397 phosphorylation in human A431 cells by ELISA
Inhibition of FAK Tyr397 phosphorylation in human A431 cells by ELISA
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[PMID: 17395594] |
| MDCK | IC50 |
500 nM
Compound: PF-228
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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
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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
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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] |
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
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CAS No. 869288-64-2
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Appearance Solid
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Molecular Weight 491.49
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Formula C22H20F3N5O3S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (39)
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Journal Impact Factor
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Most Recent
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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
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)).
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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
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
2021 Oct;35(10):e21918. PMID: 34569648 -
Cell Adh Migr
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.
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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
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 -
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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
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |