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MELK-8a hydrochloride  ≥98%

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包装规格：1mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于水(≥100mg/mL）
产品描述：基本信息 产品编号： M11673  产品名称： MELK-8a hydrochloride CAS: 2096992-20-8   储存条件 粉末 -20℃ 四年     分子式： C25H33ClN6O 溶于液体 -80℃ 6个月 分子量： 469.02 -20℃ 1个月 化学名：  1-methyl-4-(4-(4-(3-(piperidin-4-ylmethoxy)pyridin-4-yl)-1H-pyrazol-1-yl)phenyl)piperazine hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.1321mL 10.6605mL 21.3211mL 5mM 0.4264mL 2.1321mL 4.2642mL 10mM 0.2132mL 1.0661mL 2.1321mL   生物活性 产品描述 一种新颖的母体胚胎亮氨酸拉链激酶（MELK）抑制剂，其IC50值为2nM。 靶点 IC50:2nM (MELK) 体外研究 MELK-8a remains very potent (IC50=140nM) when the ATP concentration in the biochemical assay is shifted from 20μM to 2mM.Its potency is well tracked between full-length MELK versus catalytic domain construct (5nM versus 2nM).It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1μM demonstrating great selectivity.The compound is at least 90-fold more selective in targeting MELK in all cases.MELK-8a is fairly soluble (0.22g/L at pH 6.8) and shows a good permeability in the Caco-2 assay.MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2μM,respectively. 体内研究 Subcutaneous administration of MELK-8a at 30mg/kg in C57BL/6 mice results in good plasma exposure.The compound adsorption into the systemic circulation is rapid (Tmax=0.4h) and peak plasma concentration reaches 6.6μM.An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120mg/kg and all clearance mechanisms can be saturated at 240mg/kg.However,when administered orally at 10mg/kg in C57BL/6 male mice,it shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance.   推荐实验方法(仅供参考) 细胞实验:   MDA-MB-468 and MCF7 cells are seeded in growth medium into 96-well plates at 1000 and 4000 cells/well,respectively.Sixteen hours after plating,MELK-8a are added and incubated for 7 days.For each well,ATPLite reagent is added and incubated.Luminescence is measured on an multilabel plate reader.   动物实验:   Mice:For pharmacokinetic studies,the intravenous and oral dose is prepared in a solution containing 5% ethanol,100% PG,5% CremophorEL,and 80% PBS.The subcutaneous dose is formulated in 10% PG and 25% (20%,v/v) Solutol.Plasma samples are collected at specified time points and stored frozen (−20℃) until MELK-8a analysis.An LC−MS/MS method is used to quantitate MELK-8a drug levels in plasma.
保存条件：-20℃

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