GNE-7915 chemical structure
Chemical structureResearch use only
CAT. NO. DC7419Featured

GNE-7915

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Product overview

Description & Application

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

ParameterValue
Chemical Name[4-[[4-(Ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
CAS No.1351761-44-8
SynonymsGNE7915;Gne-7915;[4-[[4-(Ethylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2-fluoro-5-methoxyphenyl]-4-morpholinylmethanone;GNE 7915;[4-[[4-(Ethylamino)-5-(Trifluoromethyl)pyrimidin-2-Yl]amino]-2-Fluoranyl-5-Methoxy-Phenyl]-Morpholin-4-Yl-Methanone;GTPL8073;HMS3653J13;AOB87767;BCP09873;BDBM50398668;s7528;SB19411;BC600431;AK474042;SW219477-1;US8802674, 256;(4-((4-(ETHYLAMINO)-5-(TRIFLUOROMETHYL)PYRIMIDIN-2-YL)AMINO)-2-FLUORO-5-METHOXYPHENYL)(MORPHO;[4-[[4-(Ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-y
FormulaC19H21F4N5O3
M.Wt443.3954
SMILESFC1=C([H])C(=C(C([H])=C1C(N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O)OC([H])([H])[H])N([H])C1=NC([H])=C(C(F)(F)F)C(=N1)N([H])C([H])([H])C([H])([H])[H]
Purity98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

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].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

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