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MEK&P38 MAPK

PH-797804 (586379-66-0)

PH-797804 is an ATP-competitive, readily reversible inhibitor of the α isoform of human p38 MAP kinase, exhibiting a Ki = 5.8 nM.

Not Intended for Therapeutic Use. For research use only.

CAS: 586379-66-0 Category

PH-797804 (586379-66-0) Description:

PH-797804 is a potent and selectiove inhibitor of p38 mitogen-activated protein (MAP) kinase. PH-797804 reduces tumor growth of the three PDXs, which correlates with impaired colon tumor cell proliferation and survival. The inhibition of p38 MAPK in PDXs results in downregulation of the IL-6/STAT3 signaling pathway, which is a key regulator of colon tumorigenesis. PH-797804 may have therapeutic interest for colon cancer treatment.

PH 797804 is a member of the class of benzamides obtained by formal condensation of the carboxy group of 3-{3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1-yl}-4-methylbenzoic acid with the amino group of methylamine. It has a role as an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor and an anti-inflammatory agent. It is a member of benzamides, an organofluorine compound, a pyridone, an organobromine compound and an aromatic ether.

PH-797804 (586379-66-0) Specifications:

Product Name PH-797804
Synonym PH-797804; PH 797804; PH797804.
Chemical Name 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 586379-66-0
Molecular Formula C22H19BrF2N2O3
Molecular Weight 477.29867
Monoisotopic Mass
476.055 g/mol

 

MDL number MFCD18251426
InChIKey KCAJXIDMCNPGHZ-UHFFFAOYSA-N
InChi Code InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28)
SMILES O=C(NC)C1=CC=C(C)C(N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O)=C1
Form solid powder
Color white to beige
Solubility  Soluble in DMSO, not soluble in water.
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application PH-797804 is an orally active, potent and readily reversible ATP competitive inhibitor of the alpha isoform of human p38 MAP kinase.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Singh D, Siew L, Christensen J, Plumb J, Clarke GW, Greenaway S, Perros-Huguet C, Clarke N, Kilty I, Tan L. Oral and inhaled p38 MAPK inhibitors: effects on inhaled LPS challenge in healthy subjects. Eur J Clin Pharmacol. 2015 Oct;71(10):1175-84. doi: 10.1007/s00228-015-1920-1. Epub 2015 Aug 13. PubMed PMID: 26265232; PubMed Central PMCID: PMC4564450.
  • 2: Gupta J, Igea A, Papaioannou M, Lopez-Casas PP, Llonch E, Hidalgo M, Gorgoulis VG, Nebreda AR. Pharmacological inhibition of p38 MAPK reduces tumor growth in patient-derived xenografts from colon tumors. Oncotarget. 2015 Apr 20;6(11):8539-51. PubMed PMID: 25890501; PubMed Central PMCID: PMC4496165.
  • 3: Norman P. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. doi: 10.1517/13543784.2015.1006358. Epub 2015 Jan 20. Review. PubMed PMID: 25599809.
  • 4: Singh D. P38 inhibition in COPD; cautious optimism. Thorax. 2013 Aug;68(8):705-6. doi: 10.1136/thoraxjnl-2013-203498. Epub 2013 Apr 23. PubMed PMID: 23611882.
  • 5: MacNee W, Allan RJ, Jones I, De Salvo MC, Tan LF. Efficacy and safety of the oral p38 inhibitor PH-797804 in chronic obstructive pulmonary disease: a randomised clinical trial. Thorax. 2013 Aug;68(8):738-45. doi: 10.1136/thoraxjnl-2012-202744. Epub 2013 Mar 28. PubMed PMID: 23539534.

1 review for PH-797804 (586379-66-0)

  1. Cofttek

    Never had such good experience before,The PH-797804 (586379-66-0) is high purity,also customer service is pretty nice !gotta try!!

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