| Identification | Back Directory | [Name]
1H-3-Benzazepine, 2,3,4,5-tetrahydro-7-[2-methoxy-6-[(4-methyl-2-pyridinyl)methoxy]phenyl]- | [CAS]
1398695-47-0 | [Synonyms]
1H-3-Benzazepine, 2,3,4,5-tetrahydro-7-[2-methoxy-6-[(4-methyl-2-pyridinyl)methoxy]phenyl]- | [Molecular Formula]
C24H26N2O2 | [MOL File]
1398695-47-0.mol | [Molecular Weight]
374.48 |
| Chemical Properties | Back Directory | [Boiling point ]
517.4±50.0 °C(Predicted) | [density ]
1.122±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
10.05±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
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. DOI:10.1016/j.bmcl.2018.09.022
[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. DOI:10.1111/bph.14610 |
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