SML3853

GSK143 dihydrochloride

≥97% (HPLC)

• Synonym(s): 2-(((3R,4R)-3-Aminotetrahydro-2H-pyran-4-yl)amino)-4-(p-tolylamino)pyrimidine-5-carboxamide dihydrochloride, 2-[[(3R,4R)-3-Aminotetrahydro-2H-pyran-4-yl]amino]-4-[(4-methylphenyl)amino]-5-pyrimidinecarboxamide dihydrochloride, GSK 143 dihydrochloride, GSK-143 dihydrochloride
• Empirical Formula (Hill Notation): C₁₇H₂₂N₆O₂·2HCl
• CAS Number: 2341796-81-2
• Molecular Weight: 415.32
• MDL number: MFCD28963898
• UNSPSC Code: 12352200
• NACRES: NA.21

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: H₂O: 2 mg/mL, clear (Warmed)
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

GSK143 is an orally active, potent and selective syk inhibitor (pIC50 = 7.5 or IC50 = 31.6 nM) with good selectivity over 66 protein kinases, including 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 models, including reverse Arthus passive reaction (10 & 30 mg/kg po. in rats), postoperative ileus (POI, 1, 3 or 10 mg/kg po. in mice), and chronic HDM-induced allergic airways inflammation (30 mg/kg/day po. in mice).

Caution

Hygroscopic

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable