An orally bioavailable inhibitor of p38α MAP kinase
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Pamapimod

Item No. 20971

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(2,4-difluorophenoxy)-2-[[3-hydroxy-1-(2-hydroxyethyl)propyl]amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
CAS Number
449811-01-2
Synonyms
  • R 1503
  • Ro 4402257
Molecular Formula
C19H20F2N4O4
Formula Weight
406.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 0.33 mg/ml
λmax
222, 299, 352 nm
SMILES
FC1=CC=C(OC2=CC3=CN=C(NC(CCO)CCO)N=C3N(C)C2=O)C(F)=C1
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)
InChi Key
JYYLVUFNAHSSFE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $134

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    1 mg

    $240

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    Product Description

    Pamapimod is a potent inhibitor of p38α MAP kinase (IC50 = 14 nM).1 It displays over 30-fold selectivity for p38α over p38β, has no activity against p38δ or p38γ, and has limited activity against a panel of 350 other kinases. Pamapimod blocks LPS-induced TNF-α production by monocytes and IL-1β generation in whole blood, and it inhibits spontaneous TNF-α release from synovial explants from patients with rheumatoid arthritis.2,3 It is orally bioavailable and abrogates inflammation and bone loss in an animal model of arthritis and pain in a rat model of hyperalgesia.2 Pamapimod suppresses the expression of inflammation-associated genes in primary, IL-1β-stimulated human chondrocytes.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Goldstein, D.M., Soth, M., Gabriel, T., et al. 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. J. Med. Chem. 54(7), 2255-2265 (2011).

    2. Hill, R.J., Dabbagh, K., Phippard, D., et al. Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: Preclinical analysis of efficacy and selectivity. J. Pharmacol. Exp. Ther. 327(3), 610-619 (2008).

    3. Fehr, S., Unger, A., Schaeffeler, E., et al. Impact of p38 MAP kinase inhibitors on LPS-induced release of TNF-α in whole blood and primary cells from different species. Cell. Physiol. Biochem. 36(6), 2237-2249 (2015).

    4. Joos, H., Albrecht, W., Laufer, S., et al. Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in promary, interleukin - 1β-simulated human chondrocytes. Br. J. Pharmacol. 160(6), 1252-1262 (2010).