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Chemical Structure| 1286739-19-2 Chemical Structure| 1286739-19-2

Structure of FRAX597
CAS No.: 1286739-19-2

Chemical Structure| 1286739-19-2

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FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nM, PAK2 IC50= 13 nM, PAK3 IC50= 19 nM).

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Product Details of FRAX597

CAS No. :1286739-19-2
Formula : C29H28ClN7OS
M.W : 558.10
SMILES Code : O=C1C(C2=CC=C(C3=CN=CS3)C=C2Cl)=CC4=CN=C(NC5=CC=C(N6CCN(C)CC6)C=C5)N=C4N1CC
MDL No. :MFCD25976723
InChI Key :DHUJCQOUWQMVCG-UHFFFAOYSA-N
Pubchem ID :70934541

Safety of FRAX597

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

Related Pathways of FRAX597

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • PAK

    PAK3, IC50:13 nM

    PAK2, IC50:13 nM

  • PAK1

    PAK1, IC50:8 nM

  • PAK3

    PAK3, IC50:19 nM

  • PAK2

    PAK2, IC50:13 nM

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice T cell transfer model of chronic colitis Oral gavage 100 mg/kg QD 7 days chemical inhibition of Pak1 and Pak2 with FRAX597 suppressed active colitis in mice PMC6719711

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.79mL

0.36mL

0.18mL

8.96mL

1.79mL

0.90mL

17.92mL

3.58mL

1.79mL

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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