PF-562271
Based on 32 publication(s) in Google Scholar
PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.36%
- CAS No.: 717907-75-0
- Formula: C21H20F3N7O3S
- Molecular Weight:507.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) PF-562271
More- Nat Biomed Eng. 2025 Nov 3. [Abstract]
- Cancer Res. 2013 May 1;73(9):2873-83. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Autophagy. 2026 May 29:1-15. [Abstract]
- Carbohydr Polym. 2024 Feb 15:326:121637. [Abstract]
- Cell Discov. 2022 Sep 6;8(1):84. [Abstract]
- Clin Cancer Res. 2019 Jul 15;25(14):4552-4566. [Abstract]
- Int J Surg. 2025 Sep 17. [Abstract]
- Cell Death Dis. 2023 Feb 24;14(2):157. [Abstract]
- Cell Death Dis. 2022 Sep 10;13(9):783. [Abstract]
- Cell Rep. 2023 Oct 5;42(10):113213. [Abstract]
- Breast Cancer Res. 2024 Mar 19;26(1):48. [Abstract]
- Am J Chin Med. 2025;53(4):1225-1240. [Abstract]
- World J Gastroenterol. 2025 Jul 28;31(28):107361. [Abstract]
- Life Sci. 2021 Apr 1:270:119112. [Abstract]
- Int J Cancer. 2015 Oct 1;137(7):1549-59. [Abstract]
- Eur J Cell Biol. 2024 May 28;103(2):151427. [Abstract]
- Environ Toxicol Pharmacol. 2023 Nov:104:104301. [Abstract]
- Sci Rep. 2018 May 8;8(1):7228. [Abstract]
- Cell Signal. 2025 Sep 10:136:112117. [Abstract]
- Cancer Med. 2025 Sep;14(18):e71227. [Abstract]
- Mol Biol Rep. 2026 May 14;53(1):770. [Abstract]
- Mol Biol Rep. 2025 May 14;52(1):458. [Abstract]
- J Nat Med. 2020 Sep;74(4):732-740. [Abstract]
- Anticancer Drugs. 2024 Jan 1;35(1):46-54. [Abstract]
- Res Sq. 2025 Jul 11.
- University of Washington. 2025.
- bioRxiv. 2025 May 28.
- bioRxiv. 2025 Apr 7:2025.04.01.646098. [Abstract]
- Research Square Preprint. 2023 May 23.
- Research Square Preprint. 2021 Dec.
- Practical Oncology Journal. 2015, 29(5): 444-449.
Customer Validation & Images
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Biological Activity
IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1]
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Cell Line
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Type | Value | Description | References |
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| A375P | GI50 |
10.22 μM
Compound: PF-562271
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Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human A375P cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
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[PMID: 34324343] |
| HCT-116 | GI50 |
1.14 μM
Compound: PF-562271
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Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human HCT-116 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
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[PMID: 34324343] |
| MDA-MB-231 | GI50 |
1.95 μM
Compound: PF-562271
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Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo assay
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[PMID: 34324343] |
| Sf21 | IC50 |
13 nM
Compound: PF562271
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Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells
Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells
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[PMID: 27876318] |
| Sf9 | IC50 |
1.5 nM
Compound: PF562271
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Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP
Reversible/competitive inhibition of NH2-terminal His6-tagged FAK kinase domain (410 to 689 residues) (unknown origin) expressed in baculovirus infected sf9 cells using p(Glu/Tyr) as substrate in presence of ATP
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[PMID: 27876318] |
| SMMC-7721 | IC50 |
23.92 μM
Compound: PF-562271
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Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
Antiproliferative activity against human SMMC-7721 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay
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[PMID: 34214842] |
PF-562271 (VS-6062) is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC50 of 5 nM[1].
PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC50 of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC50 concentrations of 2.1 and 1.7 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 717907-75-0
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Appearance Solid
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Molecular Weight 507.49
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Formula C21H20F3N7O3S
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Color Light yellow to brown
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SMILES
CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O
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Synonyms
VS-6062
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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 (32)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
Nonexpansive biodegradable matrix promotes blood vessel organoid development for neurovascular repair and functional recovery in ischaemic stroke. [Abstract]2025 Nov 3. PMID: 41184604 -
Cancer Res
High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma. [Abstract]2013 May 1;73(9):2873-83. PMID: 23536552
PF-562271 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83. [Abstract]
FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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 -
Carbohydr Polym
Inulin-like polysaccharide ABWW may impede CCl4 induced hepatic stellate cell activation through mediating the FAK/PI3K/AKT signaling pathway in vitro & in vivo. [Abstract]2024 Feb 15:326:121637. PMID: 38142102 -
Cell Discov
A positive mechanobiological feedback loop controls bistable switching of cardiac fibroblast phenotype. [Abstract]2022 Sep 6;8(1):84. PMID: 36068215 -
Clin Cancer Res
High-throughput Chemical Screening Identifies Focal Adhesion Kinase and Aurora Kinase B Inhibition as a Synergistic Treatment Combination in Ewing Sarcoma. [Abstract]2019 Jul 15;25(14):4552-4566. PMID: 30979745 -
Int J Surg
Supervising the recurrence of pancreatic ductal adenocarcinoma using CtDNA-based MIR129-2 methylation detection. [Abstract]2025 Sep 17. PMID: 40961228 -
Cell Death Dis
Identification of matrix-remodeling associated 5 as a possible molecular oncotarget of pancreatic cancer. [Abstract]2023 Feb 24;14(2):157. PMID: 36828810
PF-562271 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157. [Abstract]
PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.
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Cell Death Dis
P130cas-FAK interaction is essential for YAP-mediated radioresistance of non-small cell lung cancer. [Abstract]2022 Sep 10;13(9):783. PMID: 36088346 -
Cell Rep
Mechanotransduction in response to ECM stiffening impairs cGAS immune signaling in tumor cells. [Abstract]2023 Oct 5;42(10):113213. PMID: 37804510 -
Breast Cancer Res
TMEM120B strengthens breast cancer cell stemness and accelerates chemotherapy resistance via β1-integrin/FAK-TAZ-mTOR signaling axis by binding to MYH9. [Abstract]2024 Mar 19;26(1):48. PMID: 38504374 -
Am J Chin Med
Evodiamine Suppresses Lung Cancer Progression Through Modulating FAK/STAT3/AKT Signaling Pathway. [Abstract]2025;53(4):1225-1240. PMID: 40582716 -
World J Gastroenterol
FBP1 as a key regulator of focal adhesion kinase-mediated hepatic stellate cell activation: Multi-omics and experimental validation. [Abstract]2025 Jul 28;31(28):107361. PMID: 40741470 -
Life Sci
Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway. [Abstract]2021 Apr 1:270:119112. PMID: 33508300 -
Int J Cancer
2015 Oct 1;137(7):1549-59. PMID: 25809490
PF-562271 purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59. [Abstract]
786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.
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Eur J Cell Biol
The mechanical mechanism of angiotensin II induced activation of hepatic stellate cells promoting portal hypertension. [Abstract]2024 May 28;103(2):151427. PMID: 38820882 -
Environ Toxicol Pharmacol
ZC3H4 Governs Epithelial Cell Migration through ROCK/p-PYK2/p-MLC2 Pathway in Silica-induced Pulmonary Fibrosis. [Abstract]2023 Nov:104:104301. PMID: 37866415 -
Sci Rep
The mechanical microenvironment regulates ovarian cancer cell morphology, migration, and spheroid disaggregation. [Abstract]2018 May 8;8(1):7228. PMID: 29740072 -
Cell Signal
Tenvermectin B, a novel macrocyclic lactone antibiotic, suppresses glioblastoma progression by targeting RhoJ. [Abstract]2025 Sep 10:136:112117. PMID: 40939916 -
Cancer Med
Focal Adhesion Kinase Intersects With the BRD4-MYC Axis and YAP1 to Drive Tumor Cell Growth, Phenotypic Plasticity, Stemness, and Metastatic Potential in Colorectal Cancer. [Abstract]2025 Sep;14(18):e71227. PMID: 40959971 -
Mol Biol Rep
Piperlongumine inhibits the proliferation and migration of non-small cell lung cancer cells through the EGFR/FAK/STAT3 pathway. [Abstract]2026 May 14;53(1):770. PMID: 42133146 -
Mol Biol Rep
Ginkgetin inhibits the proliferation and migration of lung cancer cells via FAK/STAT3/AKT pathway. [Abstract]2025 May 14;52(1):458. PMID: 40366441 -
J Nat Med
2020 Sep;74(4):732-740. PMID: 32643027 -
Anticancer Drugs
2024 Jan 1;35(1):46-54. PMID: 37449977 -
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bioRxiv
2025 Apr 7:2025.04.01.646098. PMID: 40291676 -
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PF-562271 purchased from MedChemExpress. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.
Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.
Solvent & Solubility
DMSO : 66.67 mg/mL (131.37 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: ≥ 1.67 mg/mL (3.29 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
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
Ewing sarcoma cells are plated in 10-cm dishes, allowed to adhere for 24 hours, and then treated with PF-562271, PD0325901, or BMS-354825. ATP content is measured as a surrogate for cell number using the CellTiter-Glo Luminescent Cell Viability Assay. Luminescence readings are obtained using the FLUOstar Omega microplate reader. For experiments with small-molecule treatment, 1.25×103 Ewing sarcoma cells are seeded in each well and treated with a range of concentrations. IC50 values are calculated from ATP measurements obtained after 3 days of treatment using log-transformed, normalized data in GraphPad Prism 5.0. Cell lines are also treated with compound in 6-cm dishes, trypsinized, and counted by light microscopy using trypan blue exclusion. For experiments using shRNA-transduced cells, 1.25×103 cells are seeded per well into 384-well plates on day 3 posttransduction. ATP content is measured on days 3, 6, and 8 posttransduction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Athymic female mice (CD-1 Nu/Nu, ~20 grams) are used for all in vivo studies. Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×106 cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of 150 mm3 in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm3) is measured with Vernier calipers and calculated using the formula: length (mm)×width (mm)×width (mm)×0.5. Percent growth inhibition. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used. A Student's t test is used to determine the P value.
Rats[3]
Nude (Crl:NIH-rnu) female rats are used. PF-562271 is formulated for oral dosing using 0.5% methyl-cellulose. On the first day of dosing, rats receive a single dose of PF-562271 (10 mg/kg) by oral gavage. Based on the exposure levels at 1 hour after dosing, the dose is reduced to 5 mg/kg. From the second day onward, rats are dosed daily with 5 mg/kg by oral gavage for 28 days. Dosing is initiated 2 weeks after tumor inoculation and only after the presence of tumors is confirmed by radiography. The presence of the tested compound in serum is confirmed during the course of the study.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 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
[1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res, 2008, 68(6), 1935-1944. [Content Brief]
[2]. Crompton BD, et al. High-throughput tyrosine kinase activity profiling identifies FAK as a candidate therapeutic target in Ewing sarcoma. Cancer Res. 2013 May 1;73(9):2873-83. [Content Brief]
[3]. Bagi CM, et al. Dual focal adhesion kinase/Pyk2 inhibitor has positive effects on bone tumors: implications for bone metastases. Cancer. 2008 May 15;112(10):2313-21. [Content Brief]
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 |
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| DMSO | 1 mM | 1.9705 mL | 9.8524 mL | 19.7048 mL | 49.2621 mL |
| 5 mM | 0.3941 mL | 1.9705 mL | 3.9410 mL | 9.8524 mL | |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9705 mL | 4.9262 mL | |
| 15 mM | 0.1314 mL | 0.6568 mL | 1.3137 mL | 3.2841 mL | |
| 20 mM | 0.0985 mL | 0.4926 mL | 0.9852 mL | 2.4631 mL | |
| 25 mM | 0.0788 mL | 0.3941 mL | 0.7882 mL | 1.9705 mL | |
| 30 mM | 0.0657 mL | 0.3284 mL | 0.6568 mL | 1.6421 mL | |
| 40 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2316 mL | |
| 50 mM | 0.0394 mL | 0.1970 mL | 0.3941 mL | 0.9852 mL | |
| 60 mM | 0.0328 mL | 0.1642 mL | 0.3284 mL | 0.8210 mL | |
| 80 mM | 0.0246 mL | 0.1232 mL | 0.2463 mL | 0.6158 mL | |
| 100 mM | 0.0197 mL | 0.0985 mL | 0.1970 mL | 0.4926 mL |
PF-562271 Related Classifications
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