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Chemical Structure| 898044-15-0 Chemical Structure| 898044-15-0

Structure of PF-3758309
CAS No.: 898044-15-0

Chemical Structure| 898044-15-0

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PF-3758309 is an inhbitor of PAKs with IC50 of 1.3 nM for PAK4, which inhbits tumor growth in HCT116, A549, M24met and other xenograft tumor models.

Synonyms: PF-03758309; PF-309

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Product Details of PF-3758309

CAS No. :898044-15-0
Formula : C25H30N8OS
M.W : 490.62
SMILES Code : O=C(N(C1)C(C)(C)C2=C1C(NC3=C4C(C=CS4)=NC(C)=N3)=NN2)N[C@@H](C5=CC=CC=C5)CN(C)C
Synonyms :
PF-03758309; PF-309
MDL No. :MFCD18633226
InChI Key :AYCPARAPKDAOEN-LJQANCHMSA-N
Pubchem ID :25227462

Safety of PF-3758309

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280

Related Pathways of PF-3758309

cytoskeleton

Isoform Comparison

Biological Activity

Description
PF-3758309 is a potent, orally bioavailable, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). It exhibits typical cellular functions associated with PAK4 inhibition, including inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].
Target
  • PAK

    PAK3, IC50:190 nM

    PAK6, Ki:17.1 nM

  • PAK1

    PAK1, Ki:13.7 nM

  • PAK3

    PAK3, IC50:99 nM

  • PAK2

    PAK2, IC50:190 nM

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00932126 Advanced Solid Tumors PHASE1 TERMINATED 2025-12-11 Pfizer Investigational Site, S... More >>anta Monica, California, 90404, United States|Pfizer Investigational Site, Aurora, Colorado, 80045, United States|Pfizer Investigational Site, East Melbourne, Victoria, 3002, Australia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.38mL

4.08mL

2.04mL

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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