DC Chemicals · Product datasheet

GNE-7915 — Datasheet

CAT. NO. DC7419

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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.

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