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Chemical Structure| 869288-64-2 Chemical Structure| 869288-64-2

Structure of PF-573228
CAS No.: 869288-64-2

Chemical Structure| 869288-64-2

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PF-573228 is an effective and selective FAK inhibitor with an IC50 of 4 nM for the purified recombinant FAK catalytic fragment.

Synonyms: FAK Inhibitor II; Focal Adhesion Kinase Inhibitor II

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Product Details of PF-573228

CAS No. :869288-64-2
Formula : C22H20F3N5O3S
M.W : 491.49
SMILES Code : O=C1NC2=C(C=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC(S(=O)(C)=O)=C4)=N3)C=C2)CC1
Synonyms :
FAK Inhibitor II; Focal Adhesion Kinase Inhibitor II
MDL No. :MFCD11519967
InChI Key :HESLKTSGTIBHJU-UHFFFAOYSA-N
Pubchem ID :11612883

Safety of PF-573228

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PF-573228

RTK
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • FAK

    FAK, IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HKC-8 cells 50 ng/ml 10 min PF-573228 inhibited FAK signaling, abolished TNC-triggered FAK and ERK1/2 activation, and suppressed fibronectin and α-SMA expression. PMC8112450
NRK-52E cells 10 µM 2 h PF-573228 inhibits FAK activity, resulting in fine cortical stress fibers and reduced LMO7 association with cortical stress fibers. PMC9741450
Retinal Ganglion Cells 10 µM 24 h To investigate the effect of the FAK inhibitor PF-573228 on BAX translocation in retinal ganglion cells. Results showed that PF-573228 induced BAX translocation after 24 h, but the percentage of translocated cells was lower compared to optic nerve injury. PMC10521527

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Acute kidney injury to chronic kidney disease model Intraperitoneal injection 5 mg/kg Once daily for 7 days PF-573228 inhibited FAK signaling, alleviated renal fibrosis, and preserved tubular integrity. PMC8112450
mice cutaneous wound model intradermal injection 15 μM once daily for 10 days To evaluate the therapeutic effect of PF-573228 on skin fibrosis, results showed that PF-573228 significantly reduced scar formation. PMC4457506
Mice Diabetic breast cancer model Subcutaneous injection 50 µM Once daily for 7 weeks Inhibition of FAK activity reduces tumor progression in diabetic mice without influencing tumor ECM stiffness. PMC9674287
Mice Optic Nerve Crush Model Intravitreal Injection 10 µM – 25 mM,1 μL Single injection, 24 hours To investigate the effect of the FAK inhibitor PF-573228 on BAX translocation in the optic nerve crush model. Results showed that PF-573228 induced BAX translocation after 24 hours, but the percentage of translocated cells was lower compared to optic nerve injury. PMC10521527

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.17mL

2.03mL

1.02mL

20.35mL

4.07mL

2.03mL

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

References

 

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