1. Cell Cycle/DNA Damage
    Cytoskeleton
    Apoptosis
  2. PAK
    Apoptosis
  3. PF-3758309 dihydrochloride

PF-3758309 dihydrochloride 

Cat. No.: HY-13007B
Handling Instructions

PF-3758309 dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

For research use only. We do not sell to patients.

PF-3758309 dihydrochloride Chemical Structure

PF-3758309 dihydrochloride Chemical Structure

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of PF-3758309 dihydrochloride:

Other Forms of PF-3758309 dihydrochloride:

Top Publications Citing Use of Products

View All PAK Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-3758309 dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].

IC50 & Target[1]

PAK4

18.7 nM (Ki)

PAK1

13.7 nM (Ki)

PAK5

18.1 nM (Ki)

PAK6

17.1 nM (Ki)

PAK2

190 nM (IC50)

PAK3

99 nM (IC50)

PAK4

2.7 nM (Kd)

In Vitro

PF-3758309 dihydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM)[1].
In cells, PF-3758309 dihydrochloride inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM)[1].
PF-3758309 dihydrochloride also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells[1].

In Vivo

PF-3758309 dihydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models[1].

Animal Model: Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)[1]
Dosage: 7.5-30 mg/kg
Administration: Oral administration; twice daily for 9-18 days
Result: Significant tumor growth inhibition (TGI) in HCT116 and A549 models.
Molecular Weight

563.55

Formula

C₂₅H₃₂Cl₂N₈OS

SMILES

CC1=NC2=C(SC=C2)C(NC3=NNC4=C3CN(C(N[[email protected]@H](C5=CC=CC=C5)CN(C)C)=O)C4(C)C)=N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PF-3758309PF3758309PF 3758309PAKApoptosisp21 activated kinasesoncogenicsignalingtumorgrowthATP-competitiveproliferationsurvivalInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-3758309 dihydrochloride
Cat. No.:
HY-13007B
Quantity:
MCE Japan Authorized Agent: