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[4-[[5-Chloro-4-(Methylamino)-2-pyrimidinyl]amino]-3-Methoxyphenyl]-4-Morpholinylmethanone

更新时间:2024-04-07 15:21:00 采购访问:37次

常用名 [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮 CAS号 1351758-81-0
价格 $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg 纯度 98.0%
备货期 需询单 库存 询单
 产品详情(用途,包装等)
用途:
HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM)IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1]Target: LRRK2HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2. HG-10-102-01 exhibited biochemical IC50s of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. At a concentration of 10 μM, HG-10-102-01 only inhibited the kinase activities of MLK1 and MNK2 to greater than 80% of the DMSO control. Dose-response analysis revealed inhibition of MLK1 with an IC50 2.1 μM and MNK2 with an IC50 0.6 μM. KinomeScan analysis against a near comprehensive panel of 451 kinases at a concentration of 1 μM resulted in no interactions detected with kinases other than G2019S LRRK2 with the exception of one mutant form of c-Kit (L576P) demonstrating the outstanding selectivity of this inhibitor.HG-10-102-01 significantly inhibited phosphorylation of wildtype LRRK2 and LRRK2[G2019S] mutant at Ser910 and Ser935 at 0.3-1.0 μM in cell culture, which is approximately the same potency as LRRK2-IN-1 (1). HG-10-102-01 is relatively insensitive to the A2016T mutation which suggests that this mutant will not be useful to validate whether the pharmacological effects of the compound are LRRK2-dependent.HG-10-102-01 can inhibit phosphorylation of Ser910 and Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 50 mg/kg. Further optimization of this chemo-type especially in regards to in vivo half-life will be reported in due course [1].
物理化学性质:
CAS号:1351758-81-0
常用中文名:[4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮
常用英文名:HG-10-102-01
分子式:C17H20ClN5O3
分子量:377.825
密度:1.4±0.1 g/cm3
沸点:641.1±65.0 °C at 760 mmHg
熔点:N/A
闪点:341.5±34.3 °C
储存条件:2-8℃

供应商信息

达阳化工(杭州)有限公司 认证供应商

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