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MEK&P38 MAPK

Pamapimod (449811-01-2)

Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor. Pamapimod inhibited p38α and p38β enzymatic activity, with IC50 values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively. Pamapimod is p38 inhibitor with IC50 of 0.06μM in THP-1 cell.

Not Intended for Therapeutic Use. For research use only.

CAS: 449811-01-2 Category

Pamapimod (449811-01-2) Description:

Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor. Pamapimod inhibited p38alpha and p38beta enzymatic activity, with IC(50) values of 0.014 +/- 0.002 and 0.48 +/- 0.04 microM, respectively. There was no activity against p38delta or p38gamma isoforms. When profiled across 350 kinases, pamapimod bound only to four kinases in addition to p38. Cellular potency was assessed using phosphorylation of heat shock protein-27 and c-Jun as selective readouts for p38 and c-Jun NH(2)-terminal kinase (JNK), respectively. Pamapimod inhibited p38 (IC(50), 0.06 microM), but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) alpha production by monocytes, interleukin (IL)-1beta production in human whole blood, and spontaneous TNFalpha production by synovial explants from RA patients. Pamapimod is a potent, selective inhibitor of p38alpha with the ability to inhibit the signs and symptoms of RA and other autoimmune diseases. (copied from J Pharmacol Exp Ther. 2008 Dec;327(3):610-9.)

Pamapimod (449811-01-2) Specifications:

Product Name Pamapimod
Synonym Pamapimod; R 1503; R1503; R-1503; Ro 4402257; Ro4402257; Ro-4402257.
Chemical Name 6-(2,4-Difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 449811-01-2
Molecular Formula C19H20F2N4O4
Molecular Weight 406.38
Monoisotopic Mass
406.145 g/mol

 

MDL number MFCD14105621
InChIKey JYYLVUFNAHSSFE-UHFFFAOYSA-N
InChi Code InChI=1S/C19H20F2N4O4/c1-25-17-11(10-22-19(24-17)23-13(4-6-26)5-7-27)8-16(18(25)28)29-15-3-2-12(20)9-14(15)21/h2-3,8-10,13,26-27H,4-7H2,1H3,(H,22,23,24)
SMILES O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
Form solid powder
Color white
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 Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

  • 1: Zhang X, Fettner S, Winter E, Masjedizadeh M, Hisoire G. Metabolism and excretion of a novel p38 MAP kinase inhibitor pamapimod in healthy male subjects. Int J Clin Pharmacol Ther. 2011 Jun;49(6):345-52. PubMed PMID: 21612741.
  • 2: Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML, Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H. Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-p yrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]py rimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. J Med Chem. 2011 Apr 14;54(7):2255-65. doi: 10.1021/jm101423y. Epub 2011 Mar 4. PubMed PMID: 21375264.
  • 3: Doggrell SA, Christensen AM. Does the p38 MAP kinase inhibitor pamapimod have potential for the treatment of rheumatoid arthritis? Expert Opin Pharmacother. 2010 Oct;11(14):2437-42. doi: 10.1517/14656566.2010.507631. PubMed PMID: 20666701.
  • 4: Zhang X, Huang Y, Navarro MT, Hisoire G, Caulfield JP. A proof-of-concept and drug-drug interaction study of pamapimod, a novel p38 MAP kinase inhibitor, with methotrexate in patients with rheumatoid arthritis. J Clin Pharmacol. 2010 Sep;50(9):1031-8. doi: 10.1177/0091270009357433. Epub 2010 Jan 25. PubMed PMID: 20100913.
  • 5: Alten RE, Zerbini C, Jeka S, Irazoque F, Khatib F, Emery P, Bertasso A, Rabbia M, Caulfield JP. Efficacy and safety of pamapimod in patients with active rheumatoid arthritis receiving stable methotrexate therapy. Ann Rheum Dis. 2010 Feb;69(2):364-7. doi: 10.1136/ard.2008.104802. Epub 2009 Apr 8. Erratum in: Ann Rheum Dis. 2011 Aug;70(8):1519. PubMed PMID: 19357113.

1 review for Pamapimod (449811-01-2)

  1. Cofttek

    Never had such good experience before,The Pamapimod (449811-01-2) is high purity,also customer service is pretty nice !gotta try!!

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