PF-3758309 | CAS 898044-15-0

PF-3758309

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
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500mg	$1150	Check With Us
1g	$1725	Check With Us

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Cat #: V1594 CAS #: 898044-15-0 Purity ≥ 99%

Description: PF-03758309 (PF03758309; PF-3758309; PF 03758309; PF3758309), a pyrrolopyrazole analog, is a novel, potent, orally bioavailable, and ATP-competitive small molecule inhibitor of PAK4 (p21-activated kinase 4) with potential antineoplastic activity.

References: Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S94

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
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Molecular Weight (MW)	490.62
Molecular Formula	C25H30N8OS
CAS No.	898044-15-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 98 mg/mL (199.7 mM)r
	Water: <1 mg/mLr
	Ethanol: 98 mg/mL (199.7 mM)
Synonyms	PF-03758309; PF-3758309; PF03758309; PF3758309; PF 03758309; PF-3758309; PF 3758309.

Protocol	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)
	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
	Animal model	Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)
	Dosages	7.5-30 mg/kg
	Administration	Oral administration; twice daily for 9-18 days

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.0382 mL	10.1912 mL	20.3824 mL	40.7647 mL
5mM	0.4076 mL	2.0382 mL	4.0765 mL	8.1529 mL
10mM	0.2038 mL	1.0191 mL	2.0382 mL	4.0765 mL
20mM	0.1019 mL	0.5096 mL	1.0191 mL	2.0382 mL

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: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.