中文名称: | WAY-600 | ||||
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英文名称: | WAY-600 | ||||
别名: | 6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-D]嘧啶;6-(1H-吲哚-5-基)-4-(4-吗啉基)-1-[1-(3-吡啶基甲基)-4-哌啶基]-1H-吡唑并[3,4-d]嘧啶;WAY 600 4-[6-(1H-Indol-5-yl)-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-4-yl]morpholine | ||||
CAS No: | 1062159-35-6 | 分子式: | C28H30N8O | 分子量: | 494.59 |
CAS No: | 1062159-35-6 | ||||
分子式: | C28H30N8O | ||||
分子量: | 494.59 |
基本信息
产品编号: |
W10071 |
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产品名称: |
WAY-600 |
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CAS: |
1062159-35-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
494.59 |
-20℃ |
1个月 |
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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 |
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Solubility (25°C): |
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体外:
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DMSO |
22mg/mL (44.48mM) |
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Ethanol |
2mg/mL (4.04mM) |
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Water |
Insoluble |
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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 |
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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。 |
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2.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:≥2.5mg/mL(5.05mM);Clear solution |
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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。 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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: |
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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: |
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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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )