GNE-0877

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP09654CAS No. ：1374828-69-9Purity：98%

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CAS No.	1374828-69-9	Cat. No.	BCP09654
Name	GNE-0877
Synonyms	GNE 0877;GNE0877;
SMILES
Chemical Name
Formula	C14H16F3N7	M. Wt	339.32
Purity	98%	Storage	Store at 4-8°C
Description	Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in the maintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension.