LRRK2-kinase inhibitor

GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.IC50 value: ~10 nM(wt-LRRK2; LRRK2 G2019S) [1]Target: LRRK2 inhibitorGSK2578215A exhibits exceptionally high selectivity for LRRK2 across the kinome, substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.3–1.0 μM in cells and in mouse spleen and kidney, but not in brain, followi

A solution of 6g (771 mg, 2.012 mmol), (2-fluoro-4-pyridinyl)boronic acid (425 mg, 3.02 mmol), bis(triphenylphosphine)palladium(II) chloride (70.6 mg, 0.101 mmol) and Na2CO3 (1066 mg, 10.06 mmol) in DME (20 mL) and water (2 mL) was stirred at reflux for 2 hours. The mixturewas then diluted with EA (50 mL) and water (50 mL). The organic layer was separated and theaqueous layer was extracted with ethyl acetate (50 mL*2). The combined organic layer wasconcentrated and the crude was purified by silica gel eluting with 0-10percent MeOH/DCM (1percentammonia) to give the title compound 8i (500 mg, 1.252 mmol, 62.2 percent yield) as an off-white solid.

Molecular Weight:399.4
XLogP3:4.1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:6
Exact Mass:399.13830499
Monoisotopic Mass:399.13830499
Topological Polar Surface Area:64.1
Heavy Atom Count:30
Complexity:543
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes