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Cat. No. M21588
GSK2646264  Structure
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Biological Activity

GSK2646264 is a potent and selective splenic tyrosine kinase (Syk) inhibitor with a pIC50 value of 7.1. GSK2646264 also inhibited other kinases, with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 for LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 penetrates into the epidermis and dermis of the skin.

Chemical Information
Molecular Weight 374.48
Formula C24H26N2O2
CAS Number 1398695-47-0
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Marion C Dickson, et al. Br J Clin Pharmacol. Effects of a topical treatment with spleen tyrosine kinase inhibitor in healthy subjects and patients with cold urticaria or chronic spontaneous urticaria: Results of a phase 1a/b randomised double-blind placebo-controlled study

[2] Alex Walker, et al. Exp Dermatol. Safety, pharmacokinetics and pharmacodynamics of a topical SYK inhibitor in cutaneous lupus erythematosus: A double-blind Phase Ib study

[3] Kirti J Johal, et al. Ann Allergy Asthma Immunol. Current and emerging treatments for chronic spontaneous urticaria

[4] Cesar Ramirez Molina, et al. Br J Pharmacol. GSK2646264, a spleen tyrosine kinase inhibitor, attenuates the release of histamine in ex vivo human skin

[5] Michael D Barker, et al. Bioorg Med Chem Lett. Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease

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Abmole Inhibitor Catalog

Keywords: GSK2646264 supplier, Syk, inhibitors, activators

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