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
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
Safety
- HS Code
- 2934999090
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.
N-Bromosuccinimide Price
- Product number
- 4279
- Product name
- PF3644022
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $315
- Updated
- 2021/12/16
- Product number
- P293825
- Product name
- PF-3644022
- Packaging
- 2.5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- 019315
- Product name
- PF-3644022
- Packaging
- 10mg
- Price
- $502
- Updated
- 2021/12/16
- Product number
- P293825
- Product name
- PF-3644022
- Packaging
- 10mg
- Price
- $675
- Updated
- 2021/12/16
- Product number
- CS-0028456
- Product name
- PF-3644022
- Purity
- >99.0%
- Packaging
- 5mg
- Price
- $595
- Updated
- 2021/12/16
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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