PF-562271 mesylate
Based on 30 publication(s) in Google Scholar
PF-562271 mesylate (VS-6062 mesylate) is an orally active, ATP-competitive, reversible FAK/Pyk2 inhibitor, with an IC50 of 1.5 nM for FAK and 13 nM for Pyk2. PF-562271 mesylate induces tumor regression, and inhibits tumor growth, invasion and metastasis. PF-562271 mesylate exerts no effect on tumor necrosis, angiogenesis or apoptosis in an orthotopic mouse model of pancreatic ductal adenocarcinoma. When combined with Sunitinib (HY-10255A), PF-562271 mesylate reduces tumor vascularization, decreases serum alpha-fetoprotein levels and improves cachexia. PF-562271 mesylate can be used in research related to prostate cancer, breast cancer, pancreatic cancer, colon cancer, glioblastoma, lung cancer, pancreatic ductal adenocarcinoma and hepatocellular carcinoma.
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- CAS No.: 939791-39-6
- Formule: C22H24F3N7O6S2
- Masse moléculaire:603.59
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) PF-562271 mesylate
More- Nat Biomed Eng. 2025 Nov 3. [Abstract]
- Cancer Res. 2013 May 1;73(9):2873-83. [Abstract]
- Autophagy. 2026 May 29:1-15. [Abstract]
- Cell Discov. 2022 Sep 6;8(1):84. [Abstract]
- Carbohydr Polym. 2024 Feb 15:326:121637. [Abstract]
- Cell Death Dis. 2023 Feb 24;14(2):157. [Abstract]
- Cell Death Dis. 2022 Sep 10;13(9):783. [Abstract]
- Clin Cancer Res. 2019 Jul 15;25(14):4552-4566. [Abstract]
- Int J Surg. 2025 Sep 17. [Abstract]
- Am J Chin Med. 2025;53(4):1225-1240. [Abstract]
- World J Gastroenterol. 2025 Jul 28;31(28):107361. [Abstract]
- Cell Rep. 2023 Oct 5;42(10):113213. [Abstract]
- Life Sci. 2021 Apr 1:270:119112. [Abstract]
- Breast Cancer Res. 2024 Mar 19;26(1):48. [Abstract]
- Sci Rep. 2018 May 8;8(1):7228. [Abstract]
- Int J Cancer. 2015 Oct 1;137(7):1549-59. [Abstract]
- Cell Signal. 2025 Sep 10:136:112117. [Abstract]
- Environ Toxicol Pharmacol. 2023 Nov:104:104301. [Abstract]
- Eur J Cell Biol. 2024 May 28;103(2):151427. [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.
- 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.
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Activité biologique
Description
In Vitro
PF-562271 mesylate potently inhibits purified recombinant FAK (with an IC50 of 1.5 nM) and recombinant Pyk2 (with an IC50 of 13 nM) via ATP-competitive reversible binding[1].
PF-562271 mesylate exhibits over 100-fold selectivity against most tested non-target recombinant kinases, and only shows moderate activity against a subset of cyclin-dependent kinase complexes[1].
PF-562271 (starting concentration of 1 μM; 30 min) mesylate potently and suppresses the autophosphorylation of FAKY397 in A431 epithelial cancer cells with an IC50 of 5 nM[1].
PF-562271 (1.1-3.3 μM; 48 h) mesylate alters the cell cycle progression of PC-3M cells only after incubation at the high concentration of 3.3 μM for 48 h[1].
PF-562271 mesylate is an ATP-competitive reversible inhibitor that potently inhibits the kinase activities of purified recombinant FAK (IC50 = 1.5 nM) and PYK2 (IC50 = 14 nM)[2].
PF-562271 (0.1 μM) mesylate significantly inhibits IGF-I-stimulated chemotactic migration of the PDA cell line MPanc-96, but does not affect EGF-stimulated migration of this cell line[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Inducible stable A431 epithelial carcinoma clones expressing wild-type V5-tagged FAK
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Concentration:1 μmol/L (starting concentration, serially diluted)
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Incubation Time:30 min
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Result:Inhibited FAKY397 autophosphorylation with an IC50 of 5 nmol/L (2.5 ng/mL).
Showed ~4-fold lower potency for Pyk2 in comparative cell assays.
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Cell Line:PC-3M human prostate cancer cells
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Concentration:1.1 μmol/L; 3.3 μmol/L
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Incubation Time:48 h
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Result:Reduced the percentage of cells in S and G2-M phases to levels comparable to serum-starved cells at 3.3 μmol/L.
Exerted no effect on cell cycle progression at 1.1 μmol/L.
In Vivo
PF-562271 (25-50 mg/kg; p.o.; once daily, twice daily; 15 days) mesylate induces dose-dependent tumor growth inhibition in PC-3M xenografts. The efficacy of twice-daily administration is superior to that of once-daily administration at the same total daily dose, and the dose of 50 mg/kg twice daily achieves a TGI of 78% accompanied by partial tumor regression[1].
PF-562271 (50-100 mg/kg; p.o.; twice daily, once daily; continuous delivery via osmotic minipump) mesylate induces significant tumor growth inhibition in BxPc3 xenografts, with the 50 mg/kg twice daily dose achieving 86% TGI and partial tumor regression[1].
PF-562271 (12.5-50 mg/kg; p.o.; twice daily; for 29 consecutive days) mesylate induces dose-dependent tumor growth inhibition in BT474 xenografts, with the 50 mg/kg twice-daily dose achieving a 94% TGI accompanied by partial tumor regression[1].
PF-562271 (33 mg/kg; twice daily) mesylate reduces tumor volume, decreases tumor cell proliferation rate, and significantly lowers the incidence of retroperitoneal invasion and metastasis of orthotopic MPanc-96 pancreatic ductal adenocarcinoma in athymic nude mice[2].
Combination treatment with PF-562271 (15 mg/kg; p.o.; twice daily; 7 days per week) mesylate and Sunitinib (HY-10255A) administered at 20 mg/kg four times daily effectively inhibits hepatocellular carcinoma tumor growth in nude mice, reduces serum AFP and AST levels, impairs tumor angiogenesis, and induces tumor necrosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 Nu/Nu (female, ≈20 grams, U87MG human glioblastoma xenograft model)[1]
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Dosage:3.3 mg/kg; 10 mg/kg; 33 mg/kg
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Administration:p.o.; single dose
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Result:Achieved 78% maximal inhibition of tumor phospho-FAK at 1 hour postdose, with >50% inhibition sustained for >4 hours (33 mg/kg dose).
Achieved 70% maximal inhibition of tumor phospho-FAK, with >50% inhibition sustained for <2 hours (10 mg/kg dose).
Calculated an EC50 of 93 ng/mL for total blood PF-562271 (mesylate) concentration required for half-maximal reduction of FAK phosphorylation.
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Animal Model:CD-1 Nu/Nu (female, ≈20 grams, PC-3M human prostate xenograft model)[1]
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Dosage:50 mg/kg (daily); 25 mg/kg (twice daily); 50 mg/kg (twice daily)
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Administration:p.o.; daily; 15 days; p.o.; twice daily; 15 days
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Result:Resulted in 45% tumor growth inhibition (TGI) and 37% inhibition of tumor phospho-FAK after 15 days, with a free Cₘₐₓ of 157 ng/mL (50 mg/kg daily dose).
Resulted in 61% TGI and 27% inhibition of tumor phospho-FAK after 15 days, with a free Cₘₐₓ of 25 ng/mL (25 mg/kg twice daily dose).
Resulted in 78% TGI, 52% inhibition of tumor phospho-FAK after 15 days, regressions in 3/7 mice, a free Cₘₐₓ of 96 ng/mL, and a free Cₐᵥₑ of 16 ng/mL (50 mg/kg twice daily dose).
Caused no weight loss, morbidity, or mortality.
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Animal Model:CD-1 Nu/Nu (female, ≈20 grams, BxPc3 human pancreatic xenograft model)[1]
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Dosage:50 mg/kg (twice daily); 100 mg/kg (daily); steady-state free concentration of 0.7 ng/mL (continuous delivery)
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Administration:p.o.; twice daily; p.o.; daily; continuous delivery via osmotic mini-pump
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Result:Resulted in 86% TGI, 31% inhibition of tumor phospho-FAK, regressions in 3/10 mice, and a free Cₘₐₓ of 273 ng/mL (50 mg/kg twice daily dose).
Resulted in 71% TGI and 59% inhibition of tumor phospho-FAK, with a free Cₘₐₓ of 705 ng/mL (100 mg/kg daily dose).
Resulted in 57% TGI and 37% inhibition of tumor phospho-FAK (continuous delivery via osmotic mini-pumps).
Caused no weight loss, morbidity, or mortality.
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Animal Model:CD-1 Nu/Nu (female, ≈20 grams, BT474 human breast xenograft model)[1]
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Dosage:12.5 mg/kg (twice daily); 25 mg/kg (twice daily); 50 mg/kg (twice daily)
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Administration:p.o.; twice daily; 29 days
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Result:Resulted in 37% TGI, 50% inhibition of tumor phospho-FAK, a free Cₘₐₓ of 29 ng/mL, and a free Cₐᵥₑ of 3 ng/mL (12.5 mg/kg twice daily dose).
Resulted in 59% TGI, 55% inhibition of tumor phospho-FAK, regressions in 3/8 mice, a free Cₘₐₓ of 116 ng/mL, and a free Cₐᵥₑ of 14 ng/mL (25 mg/kg twice daily dose).
Resulted in 94% TGI, 76% inhibition of tumor phospho-FAK, regressions in 4/8 mice, a free Cₘₐₓ of 180 ng/mL, and a free Cₐᵥₑ of 40 ng/mL (50 mg/kg twice daily dose).
Caused no weight loss, morbidity, or mortality.
Chemical Information
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CAS No. 939791-39-6
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Masse moléculaire 603.59
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Formule C22H24F3N7O6S2
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SMILES
O=C1NC2=CC=C(C=C2C1)NC3=NC=C(C(=N3)NCC4=CC=CN=C4N(C)S(=O)(=O)C)C(F)(F)F.O=S(=O)(O)C
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Synonyms
VS-6062 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (30)
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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 mesylate 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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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 -
Cell Discov
A positive mechanobiological feedback loop controls bistable switching of cardiac fibroblast phenotype. [Abstract]2022 Sep 6;8(1):84. PMID: 36068215 -
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 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 mesylate 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 -
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 -
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 -
Cell Rep
Mechanotransduction in response to ECM stiffening impairs cGAS immune signaling in tumor cells. [Abstract]2023 Oct 5;42(10):113213. PMID: 37804510 -
Life Sci
Harmine inhibits the proliferation and migration of glioblastoma cells via the FAK/AKT pathway. [Abstract]2021 Apr 1:270:119112. PMID: 33508300 -
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 -
Sci Rep
The mechanical microenvironment regulates ovarian cancer cell morphology, migration, and spheroid disaggregation. [Abstract]2018 May 8;8(1):7228. PMID: 29740072 -
Int J Cancer
2015 Oct 1;137(7):1549-59. PMID: 25809490
PF-562271 mesylate 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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Cell Signal
Tenvermectin B, a novel macrocyclic lactone antibiotic, suppresses glioblastoma progression by targeting RhoJ. [Abstract]2025 Sep 10:136:112117. PMID: 40939916 -
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 -
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 -
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 mesylate 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.
Pureté et documentation
Références
[1]. Roberts WG, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer research. 2008 Mar 15;68(6):1935-44. [Content Brief]
[2]. Stokes JB, et al. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Molecular cancer therapeutics. 2011 Nov;10(11):2135-45. [Content Brief]
[3]. Bagi CM, et al. Sunitinib and PF-562,271 (FAK/Pyk2 inhibitor) effectively block growth and recovery of human hepatocellular carcinoma in a rat xenograft model. Cancer biology & therapy. 2009 May;8(9):856-65. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-562271 mesylate Related Classifications
HY-10459A Related Classifications
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