ChemicalBook > CAS DataBase List > PF 3644022

PF 3644022

Product Name: PF 3644022
CAS No.: 1276121-88-0
Chemical Name: PF 3644022
Synonyms: PF 3644022;MK2 INHIBITOR;PF-3644022, 10 mM in DMSO;(R)-10-Methyl-3-(6-methylpyridin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one;(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;8H-[1,4]Diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one, 9,10,11,12-tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-, (10R)-;MAPKAP kinase 2,monocytic,lipopolysaccharide,IL-6,TNFα,safety,Anti-inflammatory,PF3644022,orally,PRAK,efficacious,inhibit,PF-3644022,Mitogen-activated protein kinase activated protein kinase 2,p38 MAPK,Inhibitor,MK3,MAP kinase activated protein kinase 2,MAPKAPK2 (MK2),MAPK activated protein kinase 2,PF 3644022
CBNumber: CB52596685
Molecular Formula: C21H18N4OS
Formula Weight: 374.46
MOL File: 1276121-88-0.mol

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PF 3644022 Property

Melting point:: >180°C (dec.)
Boiling point:: 703.3±60.0 °C(Predicted)
Density: 1.298±0.06 g/cm3(Predicted)
storage temp.: 2-8°C(protect from light)
solubility: DMSO (Slightly), Methanol (Slightly)
form: Solid
pka: 13.51±0.40(Predicted)
color: Off-White to Yellow

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Safety

HS Code: 2934999090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Tocris

Product number: 4279
Product name: PF3644022
Purity: ≥98%(HPLC)
Packaging: 10
Price: $315
Updated: 2021/12/16

TRC

Product number: P293825
Product name: PF-3644022
Packaging: 2.5mg
Price: $180
Updated: 2021/12/16

Usbiological

Product number: 019315
Product name: PF-3644022
Packaging: 10mg
Price: $502
Updated: 2021/12/16

TRC

Product number: P293825
Product name: PF-3644022
Packaging: 10mg
Price: $675
Updated: 2021/12/16

ChemScene

Product number: CS-0028456
Product name: PF-3644022
Purity: >99.0%
Packaging: 1mg
Price: $198
Updated: 2021/12/16

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PF 3644022 Chemical Properties,Usage,Production

Uses

PF-3644022 is a potent freely reversible ATP-competitive compound that inhibits MK2 activity (Ki = 3 nM) with good selectivity when profiled against 200 human kinases. PF-3644022 is 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.

Biological Activity

pf-3644022 is a potent and selective mitogen-activated protein kinase (mapk)-activated protein kinase-2 (mk2) inhibitor (ki =3 nm). [1]pf-3644022 is the first oral mk2 inhibitor in both acute and chronic models of inflammation. pf-3644022 reversibly atp-competitive inhibits mk2 enzyme activity with good selectivity across 200 human kinases. [1]in the human u937 monocytic cell line or peripheral blood mononuclear cells, pf-3644022 potently inhibits tnf production with ic50 value of 160 nm. in lps-stimulated human whole blood, pf-3644022 blocks tnf and il-6 production with ic50 values of 1.6 and 10.3 μm, respectively. in u937 cells and blood, inhibition of tnf correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of mk2 activity. [1]in the rat lps-induced tnf model, pf-3644022 efficacy in the chronic inflammation model is strongly correlated with maintaining a cmin higher than the ec50 measured. pf-3644022 exhibits efficaciously oral activity and good pharmacokinetic parameters in both the chronic streptococcal cell wall-induced arthritis model and the rat acute lps-induced tnf model. [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.

storage

Store at +4°C

References

1. mourey rj, burnette bl, brustkern sj 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. doi: 10.1124/jpet.110.166173. epub 2010 mar 17.

PF 3644022 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 3644022 Suppliers

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1276121-88-0, PF 3644022Related Search:

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PF 3644022

(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

MK2 INHIBITOR

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

(R)-10-Methyl-3-(6-methylpyridin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one

MAPKAP kinase 2,monocytic,lipopolysaccharide,IL-6,TNFα,safety,Anti-inflammatory,PF3644022,orally,PRAK,efficacious,inhibit,PF-3644022,Mitogen-activated protein kinase activated protein kinase 2,p38 MAPK,Inhibitor,MK3,MAP kinase activated protein kinase 2,MAPKAPK2 (MK2),MAPK activated protein kinase 2,PF 3644022

PF-3644022, 10 mM in DMSO

1276121-88-0

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