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449811-01-2,MFCD25976551
Catalog No.:AA00DB4K

449811-01-2 | PAMAPIMOD

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98+%
in stock  
$17.00   $12.00
- +
5mg
98+%
in stock  
$43.00   $30.00
- +
10mg
98+%
in stock  
$63.00   $44.00
- +
25mg
98+%
in stock  
$105.00   $74.00
- +
1g
95%
in stock  
$3,884.00   $2,719.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00DB4K
Chemical Name:
PAMAPIMOD
CAS Number:
449811-01-2
Molecular Formula:
C19H20F2N4O4
Molecular Weight:
406.3833
MDL Number:
MFCD25976551
SMILES:
OCCC(Nc1ncc2c(n1)n(C)c(=O)c(c2)Oc1ccc(cc1F)F)CCO
Properties
Computed Properties
 
Complexity:
591  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
29  
Hydrogen Bond Acceptor Count:
9  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
8  
XLogP3:
2.4  

Downstream Synthesis Route

[1]Locationinpatent:experimentalpartGoldstein,DavidM.;Soth,Michael;Gabriel,Tobias;Dewdney,Nolan;Kuglstatter,Andreas;Arzeno,Humberto;Chen,Jeffrey;Bingenheimer,William;Dalrymple,StacieA.;Dunn,James;Farrell,Robert;Frauchiger,Sandra;LaFargue,Joann;Ghate,Manjiri;Graves,Bradford;Hill,RonaldJ.;Li,Fujun;Litman,Renee;Loe,Brad;McIntosh,Joel;McWeeney,Daniel;Papp,Eva;Park,Jaehyeon;Reese,HarlanF.;Roberts,RichardT.;Rotstein,David;SanPablo,Bong;Sarma,Keshab;Stahl,Martin;Sung,Man-Ling;Suttman,RebeccaT.;Sjogren,EricB.;Tan,Yunchou;Trejo,Alejandra;Welch,Mary;Weller,Paul;Wong,BrianR.;Zecic,Hasim[JournalofMedicinalChemistry,2011,vol.54,#7,p.2255-2265]

[1]Goldstein,DavidM.;Soth,Michael;Gabriel,Tobias;Dewdney,Nolan;Kuglstatter,Andreas;Arzeno,Humberto;Chen,Jeffrey;Bingenheimer,William;Dalrymple,StacieA.;Dunn,James;Farrell,Robert;Frauchiger,Sandra;LaFargue,Joann;Ghate,Manjiri;Graves,Bradford;Hill,RonaldJ.;Li,Fujun;Litman,Renee;Loe,Brad;McIntosh,Joel;McWeeney,Daniel;Papp,Eva;Park,Jaehyeon;Reese,HarlanF.;Roberts,RichardT.;Rotstein,David;SanPablo,Bong;Sarma,Keshab;Stahl,Martin;Sung,Man-Ling;Suttman,RebeccaT.;Sjogren,EricB.;Tan,Yunchou;Trejo,Alejandra;Welch,Mary;Weller,Paul;Wong,BrianR.;Zecic,Hasim[JournalofMedicinalChemistry,2011,vol.54,#7,p.2255-2265]

[1]JournalofMedicinalChemistry,2011,vol.54,p.2255-2265

[1]Goldstein,DavidM.;Soth,Michael;Gabriel,Tobias;Dewdney,Nolan;Kuglstatter,Andreas;Arzeno,Humberto;Chen,Jeffrey;Bingenheimer,William;Dalrymple,StacieA.;Dunn,James;Farrell,Robert;Frauchiger,Sandra;LaFargue,Joann;Ghate,Manjiri;Graves,Bradford;Hill,RonaldJ.;Li,Fujun;Litman,Renee;Loe,Brad;McIntosh,Joel;McWeeney,Daniel;Papp,Eva;Park,Jaehyeon;Reese,HarlanF.;Roberts,RichardT.;Rotstein,David;SanPablo,Bong;Sarma,Keshab;Stahl,Martin;Sung,Man-Ling;Suttman,RebeccaT.;Sjogren,EricB.;Tan,Yunchou;Trejo,Alejandra;Welch,Mary;Weller,Paul;Wong,BrianR.;Zecic,Hasim[JournalofMedicinalChemistry,2011,vol.54,#7,p.2255-2265]

[1]Goldstein,DavidM.;Soth,Michael;Gabriel,Tobias;Dewdney,Nolan;Kuglstatter,Andreas;Arzeno,Humberto;Chen,Jeffrey;Bingenheimer,William;Dalrymple,StacieA.;Dunn,James;Farrell,Robert;Frauchiger,Sandra;LaFargue,Joann;Ghate,Manjiri;Graves,Bradford;Hill,RonaldJ.;Li,Fujun;Litman,Renee;Loe,Brad;McIntosh,Joel;McWeeney,Daniel;Papp,Eva;Park,Jaehyeon;Reese,HarlanF.;Roberts,RichardT.;Rotstein,David;SanPablo,Bong;Sarma,Keshab;Stahl,Martin;Sung,Man-Ling;Suttman,RebeccaT.;Sjogren,EricB.;Tan,Yunchou;Trejo,Alejandra;Welch,Mary;Weller,Paul;Wong,BrianR.;Zecic,Hasim[JournalofMedicinalChemistry,2011,vol.54,#7,p.2255-2265]

Literature

Title: Selective involvement of ERK and JNK mitogen-activated protein kinases in early rheumatoid arthritis (1987 ACR criteria compared to 2010 ACR/EULAR criteria): a prospective study aimed at identification of diagnostic and prognostic biomarkers as well as therapeutic targets.

Journal: Annals of the rheumatic diseases 20120301

Title: Metabolism and excretion of a novel p38 MAP kinase inhibitor pamapimod in healthy male subjects.

Journal: International journal of clinical pharmacology and therapeutics 20110601

Title: Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.

Journal: Journal of medicinal chemistry 20110414

Title: Tyrosine kinases in rheumatoid arthritis.

Journal: Journal of inflammation (London, England) 20110101

Title: Does the p38 MAP kinase inhibitor pamapimod have potential for the treatment of rheumatoid arthritis?

Journal: Expert opinion on pharmacotherapy 20101001

Title: A proof-of-concept and drug-drug interaction study of pamapimod, a novel p38 MAP kinase inhibitor, with methotrexate in patients with rheumatoid arthritis.

Journal: Journal of clinical pharmacology 20100901

Title: Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1beta-stimulated human chondrocytes.

Journal: British journal of pharmacology 20100701

Title: Kinase inhibitors: a new approach to rheumatoid arthritis treatment.

Journal: Current opinion in rheumatology 20100501

Title: Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.

Journal: Journal of medicinal chemistry 20100325

Title: Efficacy and safety of pamapimod in patients with active rheumatoid arthritis receiving stable methotrexate therapy.

Journal: Annals of the rheumatic diseases 20100201

Title: Optical tomographic imaging discriminates between disease-modifying anti-rheumatic drug (DMARD) and non-DMARD efficacy in collagen antibody-induced arthritis.

Journal: Arthritis research & therapy 20100101

Title: Inhibition of p38: has the fat lady sung?

Journal: Arthritis and rheumatism 20090201

Title: Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis.

Journal: Arthritis and rheumatism 20090201

Title: Clinically relevant advances in rheumatoid arthritis therapy.

Journal: F1000 medicine reports 20090101

Title: Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity.

Journal: The Journal of pharmacology and experimental therapeutics 20081201

Title: Electron paramagnetic resonance studies of actin-lipid interaction in aqueous media.

Journal: Journal of agricultural and food chemistry 19760101

Title: Hill, R. J. et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity. The Journal of pharmacology and experimental therapeutics 327, 610-619, doi:10.1124/jpet.108.139006 (2008).

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