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Chemical Structure| 717907-75-0 Chemical Structure| 717907-75-0

Structure of PF-562271
CAS No.: 717907-75-0

Chemical Structure| 717907-75-0

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PF-562271 (VS-6062) is a potent, ATP-competitive, and reversible FAK and Pyk2 kinase inhibitor with IC50 values of 1.5 nM and 13 nM, respectively.

Synonyms: VS-6062; PF-00562271

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Product Details of PF-562271

CAS No. :717907-75-0
Formula : C21H20F3N7O3S
M.W : 507.49
SMILES Code : CS(=O)(N(C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)C)=O
Synonyms :
VS-6062; PF-00562271
MDL No. :MFCD16038299
InChI Key :MZDKLVOWGIOKTN-UHFFFAOYSA-N
Pubchem ID :11713159

Safety of PF-562271

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PF-562271

RTK
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • FAK

    PYK2, IC50:13 nM

    FAK, IC50:1.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
C4-2B4 cells 5 µM PF-562271 significantly inhibited the osteocrine-induced survival of C4-2B4 cells. PMC4651787
NMuMG cells 1 μM Inhibit FAK activity, prevent EGF-induced invasion PMC3076082
PC3-mm2 cells 0.1 µM 24 h PF-562271 inhibited FAK-Y397 phosphorylation and significantly reduced the survival of PC3-mm2 cells in soft agar colony formation assays. PMC4651787
Human keratinocytes 10 µM 2 h Inhibited FAK activity, prevented the increase of p-FAK and p-Erk1/2 expression induced by JAM-A knockdown, but did not affect p-JNK expression, and slowed down keratinocyte proliferation and migration. PMC6113279
HepG2 cells 2 μM 4 h To verify whether SCBPE affects HepG2 cell proliferation through the FAK signaling pathway, results showed that PF-562271 alone or in combination with SCBPE significantly increased the cell proliferation inhibition rate. PMC11227337
Human bone marrow-derived MSCs 10 µM 6 h Inhibited FAK phosphorylation and blocked flow-induced COX2 and HO-1 expression PMC5548629
Mouse GL261 glioma cells 16 nM 72 h To evaluate the effect of PF-562271 combined with TMZ on cell viability, results showed that the combination significantly increased cell death. PMC9992029
Primary human GBM CL-3 cells 16 nM 72 h To evaluate the effect of PF-562271 combined with TMZ on cell viability, results showed that the combination significantly increased cell death. PMC9992029
Primary human GBM CL-2 cells 16 nM 72 h To evaluate the effect of PF-562271 combined with TMZ on cell viability, results showed that the combination significantly increased cell death. PMC9992029
4T1 cells 1 μM 18 h To investigate the effect of PF-562271 on FAK autophosphorylation in 4T1 cells, results showed that PF-562271 significantly inhibited FAK autophosphorylation. PMC2790843
NMuMG cells 1 μM 18 h To investigate the effect of PF-562271 on FAK autophosphorylation in NMuMG cells, results showed that PF-562271 significantly inhibited FAK autophosphorylation. PMC2790843

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice PCa-118b tumor model Oral gavage 33 mg/kg Twice a day for 2 weeks PF-562271 significantly inhibited the growth of PCa-118b tumors and delayed tumor recurrence when combined with cabozantinib. PMC4651787
Mice Aortic banding-induced cardiac hypertrophy model Oral 15 mg/kg Once daily for 3 weeks FAK inhibitor PF-562271 significantly reversed aortic banding-induced cardiac hypertrophy and fibrosis in cADAM23-KO mice PMC6222933
C57BL/6 mice C57Bl/6-GL261 glioma model Oral 50 mg/kg Once daily for 2 weeks To evaluate the effect of PF-562271 combined with TMZ on tumor growth and animal survival, results showed that the combination significantly reduced tumor size and invasive margins and increased animal survival. PMC9992029
Balb/C mice 4T1 tumor model Oral 50 mg/kg Daily, for the duration of the experiment To investigate the effect of PF-562271 on 4T1 tumor growth and lung metastasis, results showed that PF-562271 significantly reduced tumor growth and lung metastasis. PMC2790843

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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