CAS NO: | 2070015-00-6 |
生物活性 | GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor ofLRRK2with anIC50of 9 nM. | ||||||||||||||||
IC50& Target | IC50: 9 nM[1](LRRK2) | ||||||||||||||||
体外研究 (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-HT2Bwith >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2Bantagonists in vitro functional assays[2]. | ||||||||||||||||
分子量 | 615.60 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H29F4N5O6S | ||||||||||||||||
CAS 号 | 2070015-00-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(81.22 mM) *"≥" means soluble, but saturation unknown. 配制储备液
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