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PF 3644022

CAS No.
1276121-88-0
Chemical Name:
PF 3644022
Synonyms
PF 3644022;MK2 INHIBITOR;(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;(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
Molecular Weight:
374.46
MDL Number:
MFCD22683806
MOL File:
1276121-88-0.mol
MSDS File:
SDS
Last updated:2023-07-12 17:06:45

PF 3644022 Properties

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

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H320-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338
HS Code  2934999090

PF 3644022 price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Tocris 4279 PF3644022 ≥98%(HPLC) 1276121-88-0 10 $315 2021-12-16 Buy
TRC P293825 PF-3644022 1276121-88-0 2.5mg $180 2021-12-16 Buy
Usbiological 019315 PF-3644022 1276121-88-0 10mg $502 2021-12-16 Buy
TRC P293825 PF-3644022 1276121-88-0 10mg $675 2021-12-16 Buy
ChemScene CS-0028456 PF-3644022 >99.0% 1276121-88-0 5mg $595 2021-12-16 Buy
Product number Packaging Price Buy
4279 10 $315 Buy
P293825 2.5mg $180 Buy
019315 10mg $502 Buy
P293825 10mg $675 Buy
CS-0028456 5mg $595 Buy

PF 3644022 Chemical Properties,Uses,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]

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 (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 (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 1276121-88-0 Aromatics Heterocycles Inhibitors Intermediates & Fine Chemicals Pharmaceuticals