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GSK143

Chemical Structure : GSK143

CAS No.: 1240390-27-5

GSK143 (GSK-143, GSK 143)

Catalog No.: PC-63376Not For Human Use, Lab Use Only.

GSK143 is a highly potent, selective, orally efficacious Syk inhibitor with pIC50 of 7.5, >600-fold selective over ZAP-70.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK143 is a highly potent, selective, orally efficacious Syk inhibitor with pIC50 of 7.5, >600-fold selective over ZAP-70.
GSK143 inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos cells with pIC50 of 7.1, and anti-IgM induced CD69 surface expression in primary B cells with pIC50 of 6.6.
GSK143 shows good efficacy in the rat Arthus model.

Physicochemical Properties

M.Wt 342.396
Formula C17H22N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(((3R,4R)-3-aminotetrahydro-2H-pyran-4-yl)amino)-4-(p-tolylamino)pyrimidine-5-carboxamide

References

1. Liddle J, et al. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94.

2. van Bree SH, et al. Gut. 2013 Nov;62(11):1581-90.

3. Salehi S, et al. PLoS One. 2017 Jan 20;12(1):e0163614.

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