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;(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
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
5mg
Price
$595
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]

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

J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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86-10-82849933
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jkinfo@jkchemical.com
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China
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Chemsky (shanghai) International Co.,Ltd
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021-50135380
Email
shchemsky@sina.com
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China
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Wuhan TCASChem Technology Co., Ltd.
Tel
027-027-86697669 13986148687
Fax
86-027-86697669
Email
sales@tcaschem.com
Country
China
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Sichuan Wei Keqi Biological Technology Co., Ltd.
Tel
028-81700200 18116577057
Fax
028-81705658
Email
3003855609@qq.com
Country
China
ProdList
7887
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Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
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China
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EMMX Biotechnology LLC
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888-539-0666
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888-539-0666
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info@emmx.com
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United States
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8447
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Shanghai Chaolan Chemical Technology Center
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021-QQ:65489617 15618227136
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21-5161 9052
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Sales@ATKchemical.com
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China
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Shanghai SuperLan Chemcial Technique Centre
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021-2022843681 15618226720
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+86-21-51601218
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lucy@atkchemical.com
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China
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Beijing Solarbio Science & Tecnology Co., Ltd.
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010-50973130 4009686088
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3193328036@qq.com
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China
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29785
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Amadis Chemical Company Limited
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571-89925085
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0086-571-89925065
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sales@amadischem.com
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China
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1276121-88-0, PF 3644022Related Search:


  • 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
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  • Pharmaceuticals