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
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() 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 |
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
J & K SCIENTIFIC LTD. | 010-82848833 400-666-7788 | jkinfo@jkchemical.com | China | 96815 | 76 |
Chemsky (shanghai) International Co.,Ltd | 021-50135380 | shchemsky@sina.com | China | 15421 | 60 |
Wuhan TCASChem Technology Co., Ltd. | 027-027-86697669 13986148687 | sales@tcaschem.com | China | 3973 | 55 |
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