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Doramapimod

Product ID D5868
Cas No. 285983-48-4
Purity ≥99%
Product Unit SizeCostQuantityStock
10 mg $118.20 In stock
25 mg $244.40 In stock
100 mg $651.80 In stock
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  • Product Info
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  • Description
  • Product Info
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Description

Doramapimod is an anticancer chemotherapeutic inhibitor of p38 MAPK and JNK that also displays some in vitro activity against anaplastic lymphoma kinase (ALK). Doramapimod is currently in clinical trials as a potential treatment for inflammatory diseases, exhibiting anti-inflammatory activity. In vitro, this compound inhibits expression of COX-2, MMP13, iNOS, and TNF-α and decreases release of prostaglandin E2 (PGE2), decreasing the overall inflammatory response.

Product Info

Cas No.

285983-48-4

Purity

≥99%

Formula

C31H37N5O3

Formula Wt.

527.66

Chemical Name

1-(3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl)-3-(4-(2-(morpholin-4-yl)ethoxy)naphthalen-1-yl)urea

IUPAC Name

1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea

Synonym

1-[2-(4-Methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea, BIRB796

Appearance

White to off white powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

D5868 MSDS PDF

Info Sheet

D5868 Info Sheet PDF

References

Hoogendijk AJ, Pinhanços SS, van der Poll T, et al. Intrapulmonary administration of a p38 mitogen activated protein kinase inhibitor partially prevents pulmonary inflammation. Immunobiology. 2013 Apr;218(4):435-42. PMID: 22727776.

af Gennäs GB, Mologni L, Ahmed S, et al. Design, synthesis, and biological activity of urea derivatives as anaplastic lymphoma kinase inhibitors. ChemMedChem. 2011 Sep 5;6(9):1680-92. PMID: 21721129.

Kuglstatter A, Ghate M, Tsing S, et al. X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5217-20. PMID: 20655210.

Joos H, Albrecht W, Laufer S, et al. Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1beta-stimulated human chondrocytes. Br J Pharmacol. 2010 Jul;160(5):1252-62. PMID: 20590617.

Gruenbaum LM, Schwartz R, Woska JR Jr, et al. Inhibition of pro-inflammatory cytokine production by the dual p38/JNK2 inhibitor BIRB796 correlates with the inhibition of p38 signaling. Biochem Pharmacol. 2009 Feb 1;77(3):422-32. PMID: 19027720.

Kuma Y, Sabio G, Bain J, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem. 2005 May 20;280(20):19472-9. PMID: 15755732.

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