PF 3644022

Name: PF 3644022
Brand: Tocris Bioscience
SKU: 4279

Tocris Bioscience, part of Bio-Techne | Catalog # 4279

Citations (35)

COA / SDS

Potent MK2 inhibitor

Key Product Details

Description:	Potent MK2 inhibitor
Chemical Name:	(10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
Purity:	≥98% (HPLC)
Molecular Weight:	374.46

View Full Technical Details for PF 3644022

Technical Data
Citations

Biological Activity for PF 3644022

PF 3644022 is a potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC₅₀ = 5.2 nM; K_i = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC₅₀ = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 3644022 is reviewed on the chemical probes website..

Technical Data for PF 3644022

M. Wt	374.46
Formula	C₂₁H₁₈N₄OS
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1276121-88-0
PubChem ID	44631903
InChi Key	CMWRPDHVGMHLSZ-GFCCVEGCSA-N
Smiles	O=C(N[C@H](C)CN4)C3=C4C1=C(S3)C=CC2=C1C=CC(C5=CC=C(C)N=C5)=N2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PF 3644022

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	14.98	40

Preparing Stock Solutions for PF 3644022

The following data is based on the product molecular weight 374.46.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.4 mM	6.68 mL	33.38 mL	66.76 mL
2 mM	1.34 mL	6.68 mL	13.35 mL
4 mM	0.67 mL	3.34 mL	6.68 mL
20 mM	0.13 mL	0.67 mL	1.34 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for PF 3644022

References are publications that support the biological activity of the product.

Mourey A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J.Pharmacol.Exp.Ther. 2010 PMID: 20237073