GNE-7915 tosylate (C007B-357962)

GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC 50 of 9 nM.In VitroMaintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 μM for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE-7915 at 0.1 μM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT 2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT 2B antagonists in vitro functional assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 9 nM,(LRRK2). Specification: 0.99 Molecular Formula: C26H29F4N5O6S Molecular Weight: 615.6 PubChem CID: 78357832 Isomeric SMILES: CCNC1=NC(=NC=C1C(F)(F)F)NC2=C(C=C(C(=C2)F)C(=O)N3CCOCC3)OC.CC1=CC=C(C=C1)S(=O)(=O)O

UPC:

51202701

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

G651430-10mg

CAS:

2070015-00-6

Product Size:

10mg