Home Tools

Cart

PF-3758309

Catalog No. T6626 CAS 898044-15-0

Synonyms: PF 3758309, PF-309, PF-03758309, PF3758309

PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

PF-3758309, CAS 898044-15-0

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-03758309 (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.
Targets&IC50	PAK3:99 nM, PAK6:17.1 nM(Ki), PAK4:1.3 nM, PAK4:18.7 nM(Ki), PAK5:18.1 nM(Ki)
In vitro	PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 （Ki=18.7 nM）, has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM.
In vivo	In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts.
Kinase Assay	In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921).
Cell Research	HEK293T, HCT116, and SKOV3 cells are plated on 384-well plates for 24 hours culture. PF-3758309( ~1 μM) is added to the cell culture incubating 72 hours. After drug treatment,cell proliferation and other indicators of metabolism are measured.
Animal Research	Nude mice with Xenograft tumors were orally fed with PF-3758309（7.5-30 mg/kg BID）dissolved in 0.5% methylcellulose.

Synonyms	PF 3758309, PF-309, PF-03758309, PF3758309
Molecular Weight	490.63
Formula	C25H30N8OS
CAS No.	898044-15-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 91 mg/mL (185.5 mM)

Ethanol: 91 mg/mL (185.5 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Murray BW, et al. Proc Natl Acad Sci U S A, 2010, 107(20), 9446-9451.

Related Products

Related compounds with same targets

(S)-(−)-Perillyl alcohol CPI-360 Diclofenac Potassium PF-543 GSK1904529A Ezatiostat LYN-1604 Curzerene

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-3758309 898044-15-0 凋亡细胞骨架 Apoptosis PAK proliferation tumor oncogenic PF 3758309 survival PF03758309 PF3758309 inhibit p21 activated kinases signaling PF-309 ATP-competitive Inhibitor PF 03758309 PF-03758309 growth inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.