1351761-44-8
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
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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 | |
| 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 |
| 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℃ |