PF 3644022

Modify Date: 2024-04-03 15:45:52

PF 3644022 Structure
PF 3644022 structure
 Common Name PF 3644022
CAS Number 1276121-88-0 Molecular Weight 374.45900
Density N/A Boiling Point N/A
Molecular Formula C21H18N4OS Melting Point N/A
MSDS USA Flash Point N/A

 Use of PF 3644022


PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect[1].

 Names

Name (10R)-10-Methyl-3-(6-methyl-3-pyridinyl)-9,10,11,12-tetrahydro-8H -[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
Synonym More Synonyms

 PF 3644022 Biological Activity

Description PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect[1].
Related Catalog
Target

IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3)[1]. Ki: 3 nM (MK2)[1]

In Vitro The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1]. In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity[1].
In Vivo PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED50 value of 20 mg/kg[1]. Animal Model: Female Lewis rats (125-140 g) injected with streptococcal cell wall[1] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg Administration: Oral gavage; twice a day; for 12 days Result: Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
References

[1]. Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807

 Chemical & Physical Properties

Molecular Formula C21H18N4OS
Molecular Weight 374.45900
Exact Mass 374.12000
PSA 98.64000
LogP 4.51210

 Safety Information

Hazard Codes Xi

 Synonyms

8-Aminoadenine
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Chemsrc provides PF 3644022(CAS#:1276121-88-0) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of PF 3644022 are included as well.>> amp version: PF 3644022

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