| Identification | Back Directory | [Name]
R1487 | [CAS]
449808-64-4 | [Synonyms]
R1487
CS-667
RI-487
CS-2169
SY-R1487
R1487 HCL
R-1487;R 1487
R1487 (Hydrochloride)
R1487 (SY-R1487)
R-1487 HYDROCHLORIDE;R 1487 HYDROCHLORIDE
6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-difluorophenoxy)-8-Methyl-2-[(tetrahydro-2H-pyran-4-yl)aMino]-, (Hydrochloride) (1:1) | [Molecular Formula]
C19H19ClF2N4O3 | [MOL File]
449808-64-4.mol | [Molecular Weight]
424.829 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml | [form ]
A crystalline solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively[1]. | [in vivo]
R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β[1].
Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively[1].
| [IC 50]
p38α: 0.2 nM (Kd); p38β: 29 nM (Kd) | [storage]
Store at -20°C | [References]
[1] Goldstein DM 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. 2011 Apr 14;54(7):2255-65. DOI:10.1021/jm101423y |
|
|