GSK2646264_product_DataBase

Bioactivity	GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].
Invitro	GSK2646264 (0.01-10 μM; 1 h) significantly inhibits anti‐IgE (but not C5a)‐induced histamine release from skin mast cells in a concentration‐dependent manner. The IC50 is 0.7 μM and the IC90 is 6.8 μM[2].GSK2646264 cream (0.5, 1, and 3% [wt/wt]; 1 cm2; 4 and 24 h) inhibits anti‐IgE‐induced histamine release from mast cells in ex vivo human skin[2].
Name	GSK2646264
CAS	1398695-47-0
Formula	C24H26N2O2
Molar Mass	374.48
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Barker MD, et al. Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3458-3462. [2]. Ramirez Molina C, et al. GSK2646264, a spleen tyrosine kinase inhibitor, attenuates the release of histamine in ex vivo human skin. Br J Pharmacol. 2019 Apr;176(8):1135-1142.

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