| Identification | Back Directory | [Name]
5-Pyrimidinecarboxamide, 2-[[(3R,4R)-3-aminotetrahydro-2H-pyran-4-yl]amino]-4-[(4-methylphenyl)amino]-, hydrochloride (1:2) | [CAS]
2341796-81-2 | [Synonyms]
GSK143 dihydrochloride
5-Pyrimidinecarboxamide, 2-[[(3R,4R)-3-aminotetrahydro-2H-pyran-4-yl]amino]-4-[(4-methylphenyl)amino]-, hydrochloride (1:2) | [Molecular Formula]
C17H23ClN6O2 | [MOL File]
2341796-81-2.mol | [Molecular Weight]
378.86 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, away from moisture and light | [solubility ]
Soluble to 100 mM in water and to 100 mM in DMSO | [form ]
Solid | [color ]
Off-white to light yellow | [Water Solubility ]
H2O: 2mg/mL, clear (Warmed) |
| Hazard Information | Back Directory | [Biological Activity]
GSK143 is an orally activepotent and selective syk inhibitor (pIC50 = 7.5 or IC50 = 31.6 nM) with good selectivity over 66 protein kinasesincluding ZAP-70 (pIC50 = 4.7 or IC50 = 20 μM). GSK143 effectively inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos cells (pIC50 = 7.1 or IC50 = 79.4 nM) and demonstrates in vivo efficacy in animal inflammatory disease modelsincluding reverse Arthus passive reaction (10 & 30 mg/kg po. in rats)postoperative ileus (POI13 or 10 mg/kg po. in mice)and chronic HDM-induced allergic airways inflammation (30 mg/kg/day po. in mice). | [storage]
Store at -20°C |
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