R1487 (hydrochloride)

R1487 is an inhibitor of p38alpha MAPK (IC50 = 10 nM). It is selective for p38alpha over p38beta 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-1beta production in isolated human whole blood (IC50 = 170 nM). It also inhibits LPS-induced production of TNF-alpha 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).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: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 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.