An inhibitor of p38α MAPK
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R1487 (hydrochloride)

Item No. 31478

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(2,4-difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-pyrido[2,3-d]pyrimidin-7(8H)-one, monohydrochloride
CAS Number
449808-64-4
Molecular Formula
C19H18F2N4O3 • HCl
Formula Weight
424.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
299, 349 nm
SMILES
O=C1C(OC2=CC=C(C=C2F)F)=CC3=C(N1C)N=C(NC4CCOCC4)N=C3.Cl
InChi Code
InChI=1S/C19H18F2N4O3.ClH/c1-25-17-11(10-22-19(24-17)23-13-4-6-27-7-5-13)8-16(18(25)26)28-15-3-2-12(20)9-14(15)21;/h2-3,8-10,13H,4-7H2,1H3,(H,22,23,24);1H
InChi Key
RQHSAIGGUWVOBG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $293

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    25 mg

    $437

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    Product Description

    R1487 is an inhibitor of p38α MAPK (IC50 = 10 nM).1 It is selective for p38α over p38β MAPK (Kds = 0.2 and 29 nM, respectively), as well as a panel of 306 additional kinases at 10 µM, but does inhibit 11 kinases by greater than 85% at 10 µM. R1487 inhibits LPS-induced IL-1β production in isolated human whole blood (IC50 = 170 nM). It also inhibits LPS-induced production of TNF-α and IL-6 in rats (ED50s = 0.8 and 0.4 mg/kg). R1487 reduces yeast-induced hyperalgesia in rats (ED50 = 5.5 mg/kg).

    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).