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

PF-3758309  (Synonyms: PF-03758309)

Cat. No.: HY-13007 Purity: 99.84%
COA Handling Instructions

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 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 Chemical Structure

PF-3758309 Chemical Structure

CAS No. : 898044-15-0

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 73 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of PF-3758309:

Top Publications Citing Use of Products

View All PAK Isoform Specific Products:

View All Isoforms
PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 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 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 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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

PF-3758309 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

490.62

Appearance

Solid

Formula

C25H30N8OS
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (203.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0382 mL 10.1912 mL 20.3824 mL
5 mM 0.4076 mL 2.0382 mL 4.0765 mL
10 mM 0.2038 mL 1.0191 mL 2.0382 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.84%

COA (256 KB) HNMR (440 KB) RP-HPLC (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

PF-3758309898044-15-0PF-03758309PF3758309PF 3758309PF03758309PF 03758309PAKApoptosisp21 activated kinasesoncogenicsignalingtumorgrowthATP-competitiveproliferationsurvivalInhibitorinhibitorinhibit

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