DC Chemicals Limited
China
Product Name: GNE-7915
Price: $400.0/100mg $800.0/250mg $1700.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1351761-44-8

1351761-44-8 structure

1351761-44-8 structure

Name: GNE7915
Chemical Name: gne-7915
CAS Number: 1351761-44-8
Molecular Formula: C₁₉H₂₁F₄N₅O₃
Molecular Weight: 443.395
Catalog: Biochemical Inhibitor Autophagy lysosome (Autophagy) LRRK2 inhibitor
Create Date: 2016-04-06 14:47:44
Modify Date: 2024-01-04 09:39:30
GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

Name	gne-7915
Synonyms	gne 7915 (4-{[4-(Ethylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino}-2-fluoro-5-methoxyphenyl)(4-morpholinyl)methanone Methanone, [4-[[4-(ethylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2-fluoro-5-methoxyphenyl]-4-morpholinyl-

Description	GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
Related Catalog	Signaling Pathways >> Autophagy >> LRRK2 Research Areas >> Neurological Disease
Target	IC50: 9 nM[1] (LRRK2)
In Vitro	Maintaining 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-HT2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitro functional assays[2].
References	[1]. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6. [2]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33.

Density	1.4±0.1 g/cm3
Boiling Point	629.9±65.0 °C at 760 mmHg
Molecular Formula	C₁₉H₂₁F₄N₅O₃
Molecular Weight	443.395
Flash Point	334.7±34.3 °C
Exact Mass	443.158051
PSA	88.61000
LogP	1.81
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.578
Storage condition	2-8℃