2. Protein Tyrosine Kinase/RTK
  3. FAK Pyk2
  4. PF-562271 mesylate

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

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PF-562271 mesylate Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    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.

    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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    Description

    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[1][2][3].

    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.

    PF-562271 mesylate Related Antibodies

    ELISA Assay[1]

    Cell Line: Inducible stable A431 epithelial carcinoma clones expressing wild-type V5-tagged FAK
    Concentration: 1 μmol/L (starting concentration, serially diluted)
    Incubation Time: 30 min
    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.

    Cell Cycle Analysis[1]

    Cell Line: PC-3M human prostate cancer cells
    Concentration: 1.1 μmol/L; 3.3 μmol/L
    Incubation Time: 48 h
    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 (3.3-33 mg/kg; p.o.; single dose) mesylate inhibits tumor FAK phosphorylation in a dose- and time-dependent manner after oral administration, with an EC50 of 93 ng/mL for whole blood concentrations[1].
    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.

    Animal Model: CD-1 Nu/Nu (female, ≈20 grams, U87MG human glioblastoma xenograft model)[1]
    Dosage: 3.3 mg/kg; 10 mg/kg; 33 mg/kg
    Administration: p.o.; single dose
    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.
    Animal Model: CD-1 Nu/Nu (female, ≈20 grams, PC-3M human prostate xenograft model)[1]
    Dosage: 50 mg/kg (daily); 25 mg/kg (twice daily); 50 mg/kg (twice daily)
    Administration: p.o.; daily; 15 days; p.o.; twice daily; 15 days
    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.
    Animal Model: CD-1 Nu/Nu (female, ≈20 grams, BxPc3 human pancreatic xenograft model)[1]
    Dosage: 50 mg/kg (twice daily); 100 mg/kg (daily); steady-state free concentration of 0.7 ng/mL (continuous delivery)
    Administration: p.o.; twice daily; p.o.; daily; continuous delivery via osmotic mini-pump
    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.
    Animal Model: CD-1 Nu/Nu (female, ≈20 grams, BT474 human breast xenograft model)[1]
    Dosage: 12.5 mg/kg (twice daily); 25 mg/kg (twice daily); 50 mg/kg (twice daily)
    Administration: p.o.; twice daily; 29 days
    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.
    Molecular Weight

    603.59

    Formula

    C22H24F3N7O6S2
    CAS No.
    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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    PF-562271 mesylate Related Classifications

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    • Do most proteins show cross-species activity?

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    Keywords:

    PF-562271939791-39-6VS-6062PF562271PF 562271VS6062VS 6062FAKPyk2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2tyrosine kinaseprostate cancerMAD08-608 human PDA cell linebreast cancerPC-3M human prostate cancer cellA431 epithelial carcinoma cellspancreatic ductal adenocarcinomaMPanc-96 human PDA cell lineInhibitorinhibitorinhibit

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