SML3853
GSK143 dihydrochloride
≥97% (HPLC)
别名:
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
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关于此项目
经验公式（希尔记法）:
C17H22N6O2·2HCl
化学文摘社编号:
分子量:
415.32
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
form
powder
assay
≥97% (HPLC)
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear (Warmed)
storage temp.
-10 to -25°C
Quality Level
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).
Orally active, potent and highly selective syk inhibitor with in vivo efficacy in animal inflammatory disease models.
Disclaimer
Hygroscopic
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Syk Regulates Neutrophilic Airway Hyper-Responsiveness in a Chronic Mouse Model of Allergic Airways Inflammation
PLoS ONE, 12(1), e0163614-e0163614 (2017)
Inhibition of spleen tyrosine kinase as treatment of postoperative ileus
Gut, 62(11), 1581-1590 (2013)
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor
Bioorganic & Medicinal Chemistry Letters, 21(20), 6188-6194 (2011)
Highly selective SYK inhibitor, GSK143, abrogates survival signals in chronic lymphocytic leukaemia
British Journal of Haematology, 182(6), 927-930 (2018)
Christine Braegelmann et al.
Experimental dermatology, 25(5), 375-379 (2016-02-26)
Spleen tyrosine kinase (SYK) is a protein kinase involved in cell proliferation and the regulation of inflammatory pathways. Due to the increasing evidence that kinase inhibitors have potential as specific anti-inflammatory drugs, we have investigated the potential for SYK inhibition
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