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SML3853

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C17H22N6O2·2HCl
CAS Number:
Molecular Weight:
415.32
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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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)
Syk Regulates Neutrophilic Airway Hyper-Responsiveness in a Chronic Mouse Model of Allergic Airways Inflammation
PLoS ONE, 12(1), e0163614-e0163614 (2017)
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
Highly selective SYK inhibitor, GSK143, abrogates survival signals in chronic lymphocytic leukaemia
British Journal of Haematology, 182(6), 927-930 (2018)

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