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AX-15836  ≥98%

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包装规格：2mg 5mg 10mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(100mg/ml超声）
产品描述：基本信息 产品编号： A12281 产品名称： AX-15836 CAS: 2035509-96-5   储存条件 粉末 -20℃ 四年     分子式： C32H40N8O5S 溶于液体 -80℃ 六个月 分子量 648.78 -20℃ 一个月 化学名：  2-(2-Ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenylamino)-5-methyl-11-(methylsulfonyl)-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one Solubility (25°C)：   体外:   DMSO 100mg/mL(154.14mM;Need ultrasonic) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline，Solubility:≥2.5mg/mL(3.85mM);Clear solution 此⽅案可获得≥2.5mg/mL(3.85mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到400μLPEG300中，混合均匀；向上述体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.5mg/mL(3.85mM);Clear solution 此⽅案可获得≥2.5mg/mL(3.85mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution 此⽅案可获得≥2.5mg/mL(3.85mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 ＜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 1.5414mL 7.7068mL 15.4135mL 5mM 0.3083mL 1.5414mL 3.0827mL 10mM 0.1541mL 0.7707mL 1.5414mL   生物活性 产品描述 一种有效的选择性的ERK5抑制剂，IC50值为8nM。 靶点 ERK5 8nM(IC50) 体外研究 AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a Kd of 3,600nM. AX15836 shows similar intracellular potency (4–9nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. AX15836 was completely ineffective (EC50>10μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells   推荐实验方法(仅供参考) Cell Assay For proliferation studies, cells are treated with eight-point serial dilution series of AX-15836 (starting concentration of 15μM) or with DMSO vehicle (0.25% final volume). For MM.1S cells, compound was added 1 h before adding recombinant human IL6 at 5nM. After 3 d, the relative number of viable cells was measured via quantitation of ATP using CellTiter-Glo 2.0 reagent. Luminescence was read on the Synergy 2 multimode reader
保存条件：-20℃

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