GSK2646264

Names

[ Name ]:
GSK2646264

[Synonym ]:
7-{2-Methoxy-6-[(4-methyl-2-pyridinyl)methoxy]phenyl}-2,3,4,5-tetrahydro-1H-3-benzazepine
1H-3-Benzazepine, 2,3,4,5-tetrahydro-7-[2-methoxy-6-[(4-methyl-2-pyridinyl)methoxy]phenyl]-

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Aurora Kinase

Signaling Pathways >> Stem Cell/Wnt >> GSK-3

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Signaling Pathways >> JAK/STAT Signaling >> JAK

Signaling Pathways >> Epigenetics >> JAK

Signaling Pathways >> Stem Cell/Wnt >> JAK

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src

Signaling Pathways >> Autophagy >> LRRK2

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Syk

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

SYK:7.1 (pIC50)

LCK:5.4 (pIC50)

LRRK2:5.4 (pIC50)

GSK3β:5.3 (pIC50)

JAK2:5 (pIC50)

VEGFR2:4.5 (pIC50)

Aurora B:<4.6 (pIC50)

Aurora A:<4.3 (pIC50)

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
517.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₆N₂O₂

[ Molecular Weight ]:
374.48

[ Flash Point ]:
266.7±30.1 °C

[ Exact Mass ]:
374.199432

[ LogP ]:
3.40

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.585