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    PF-562271 HCl
    PF-562271 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0660
    CAS #: 939791-41-0 Purity ≥98%

    Description: PF-562271 HCl is the hydrochloride salt of PF-562271, PF-562271 is a potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 (proline-rich tyrosine kinase) catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively. it has >100-fold selectivity against other protein kinases. Additionally, PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5 nmol/L. PF-562,271 was evaluated against multiple kinases and displays >100x selectivity against a long list of nontarget kinases. PF-562,271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC(50) of 93 ng/mL, total) after p.o. administration to tumor-bearing mice. In vivo inhibition of FAK phosphorylation (>50%) was sustained for >4 hours with a single p.o. dose of 33 mg/kg. Antitumor efficacy and regressions were observed in multiple human s.c. xenograft models. PF-562271 is a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer.  

    References: Cancer Res. 2008 Mar 15;68(6):1935-44; Cancer Biol Ther. 2010 Jul 1;10(1):38-43.

    Related CAS: 939791-41-0 (HCl); 717907-75-0 (free base); 939791-39-6 (mesylate); 939791-40-9 (tosylate); 939791-38-5 (besylate)

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    Molecular Weight (MW)543.95
    FormulaC21H21ClF3N7O3S
    CAS No.939791-41-0 (HCl); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (183.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.[H]Cl
    SynonymsPF562271 HCl; PF562271 hydrochloride; PF 562271; PF562271; PF-562271; PF-00562271; PF00562271; PF 00562271; PF00562271 hydrochloride. PF271; PF-271; PF 271; 

    InChi Key: RQEBZJWSAAWCAV-UHFFFAOYSA-N

    InChi Code: InChI=1S/C21H20F3N7O3S.ClH/c1-31(35(2,33)34)19-12(4-3-7-25-19)10-26-18-15(21(22,23)24)11-27-20(30-18)28-14-5-6-16-13(8-14)9-17(32)29-16;/h3-8,11H,9-10H2,1-2H3,(H,29,32)(H2,26,27,28,30);1H

    SMILES Code: CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.[H]Cl


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    In Vitro

    In vitro activity: PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels.


    Kinase Assay: PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively.


    Cell Assay: Cells (Squamous cell carcinoma (SCC) are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.

    In VivoPF-562271 (< 33 mg/kg p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in U87MG-bearing mice. PF-562271 (50 mg/kg p.o. bid) results in 86% tumor growth inhibition in BxPc3 xenografts mice and 45% tumor growth inhibition in PC3-M xenografts mice. PF-562271 (25 mg/kg, bid) results in 2-fold greater apoptosis in treated tumors in mice bearing H125 lung xenografts. PF-562271 (33 mg/kg, p.o.) inhibits extensive movement of the tumor cells over 24 hours in mice. PF-562271 (33 mg/kg, p.o.) results in altered E-cadherin dynamics in mice, which correlates with reduced E-cadherin–dependent collective cell movement. PF-562271 (25 mg/kg, p.o. bid) results in 62% tumor growth inhibition in PC3M-luc-C6 subcutaneuous local implant xenograft mouse model. PF-562,271 (5 mg/kg, oral) results in significant and similar increases in osteocalcin and cancellous bone parameters and a decrease in tumor growth and signs of bone healing in rats implanted with MDA-MB-231 cells in the tibia.
    Animal modelAthymic female mice bearing BxPc3 or PC3-M xenografts.
    Formulation & DosageDissolved in in 5% Gelucire; 100 mg/kg; Oral gavage
    References

    Cancer Res. 2008 Mar 15;68(6):1935-44; Cancer Biol Ther. 2010 Jul 1;10(1):38-43.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-562271 HCl

    Efficacy of PF-562,271 in PC3M-luc-C6 subcutaneuous local implant xenograft model: PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. Cancer Biol Ther. 2010 Jul 1;10(1):38-43.

    PF-562271 HCl

    (A) Bioluminescent image time course of a subcutaneously inoculated vehicle control mouse. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. (B) Bioluminescent image time course of a subcutaneously inoculated mouse treated with PF-562,271. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. Cancer Biol Ther.2010 Jul 1;10(1):38-43.

    PF-562271 HCl

    (A) Bioluminescent image time course of an intracardiac inoculated vehicle control mouse. Vehicle was administered P.O. BID 5x/wk for three weeks. (B) Bioluminescent image time course of an intracardiac inoculated treated with PF-562,271. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for three weeks. Cancer Biol Ther. 2010 Jul 1; 10(1): 38–43.


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