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WAY-600  ≥95%

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包装规格：2mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(50mg/mL超声）
产品描述：基本信息 产品编号： W10071 产品名称： WAY-600 CAS: 1062159-35-6   储存条件 粉末 -20℃ 四年     分子式： C28H30N8O 溶于液体 -80℃ 6个月 分子量： 494.59 -20℃ 1个月 化学名：  4-[6-(1H-Indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine Solubility (25°C)：   体外:   DMSO 22mg/mL (44.48mM) Ethanol 2mg/mL (4.04mM) Water Insoluble 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(5.05mM);Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.05mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-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% corn oil Solubility:≥2.5mg/mL(5.05mM);Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.05mM，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 100μL 25.0 mg/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 2.0219mL 10.1094mL 20.2188mL 5mM 0.4044mL 2.0219mL 4.0438mL 10mM 0.2022mL 1.0109mL 2.0219mL   生物活性 产品描述 一种有效，ATP竞争型，选择性的mTOR抑制剂，抑制重组mTOR酶的IC50值为9nM。WAY-600阻断mTOR复合物1/2(mTORC1/2)组装和激活。 靶点 mTOR   体外研究 WAY-600 exhibits a concentration-dependent and time-dependent inhibition of f HepG2 and Huh-7 cells viability.Following WAY-600 (1-1000nM) treatment,the number of HepG2 cell colonies is dramatically decreased.Meanwhile,BrdU incorporation in HepG2 cells is also inhibited with WAY-600 treatment.WAY-600 dose-dependently increases the activity of caspase-3 and caspase-9 in HepG2 cells.WAY-600 disrupts assemble of mTORC1 (mTOR-Raptor association) and mTORC2 (mTOR-Rictor association).Activation of mTORC1 (indicated by p-S6K1 and p-4E-BP1) and mTORC2 is almost blocked by WAY-600 (100nM). 体内研究 Administration of WAY-600 (10mg/kg,daily) inhibits HepG2 tumor growth in nude mice.Daily HepG2 tumor growth of WAY600-administrated mice is significantly lower than that of vehicle control mice.Importantly,the in vivo anti-cancer activity by WAY-600 is further potentiated with the co-administration of MEK-162 (2.5mg/kg,p.o.daily).   推荐实验方法(仅供参考) 细胞实验:   Established HCC cells (HepG2 and Huh-7),primary HCC cells (Pnt-1/-2/-3/-4),or THLE-2 liver cells are cultured in WAY-600 (1-1000nM)-containing medium for 24,48,72,96 hours,cell viability is tested by MTT assay.   动物实验:   Mice:Mice tumor xenografts are randomly divided into four groups (10 mice per group):vehicle (intraperitoneal or i.p.),WAY-600 (10mg/kg,i.p.injection),MEK-162 (2.5mg/kg,oral gavage) or WAY-600 plus MEK-162 combination.The mice are monitored for activity and physical condition on daily basis,and mice body weights and tumor mass are measured weekly.
保存条件：-20℃

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