中文名称: | 冬凌草甲素 | ||||
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英文名称: | Oridonin | ||||
别名: | 冬凌草甲素 (14R)-7-alpha,20-Epoxy-1-alpha,6-beta,7,14-tetrahydroxykaur-16-en-15-one | ||||
CAS No: | 28957-04-2 | 分子式: | C20H28O6 | 分子量: | 364.43 |
CAS No: | 28957-04-2 | ||||
分子式: | C20H28O6 | ||||
分子量: | 364.43 | ||||
MDL: | MFCD00221762 |
基本信息
产品编号: |
O10559 |
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产品名称: |
Oridonin |
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CAS: |
28957-04-2 |
储存条件 |
粉末 |
2-8℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
364.43 |
-20℃ |
一个月 |
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化学名: |
(14R)-7-alpha,20-Epoxy-1-alpha,6-beta,7,14-tetrahydroxykaur-16-en-15-one |
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Solubility (25°C): |
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体外:
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DMSO |
73mg/mL (200.31mM) |
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Ethanol |
28mg/mL (76.83mM) |
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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% 1-Methyl-2-pyrrolidinone→90% PEG300 Solubility: ≥ 5mg/mL (13.72mM); Clear solution 2.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution |
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此⽅案可获得 ≥ 2.08mg/mL (5.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 20.8mg/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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3.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution |
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此⽅案可获得 ≥ 2.08mg/mL (5.71mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 20.8mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。 |
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4.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility: ≥ 2.08mg/mL (5.71mM); Clear solution |
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此⽅案可获得 ≥ 2.08mg/mL (5.71mM,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 20.8mg/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 |
2.7440mL |
13.7201mL |
27.4401mL |
5mM |
0.5488mL |
2.7440mL |
5.4880mL |
10mM |
0.2744mL |
1.3720mL |
2.7440mL |
50mM |
0.0549mL |
0.2744mL |
0.5488mL |
生物活性
产品描述 |
Oridonin (Isodonol, Rubescenin, NSC-250682) 是从Rabdosia rubescens中分离的对映贝壳杉烷二萜,是一种具有抗肿瘤、抗细菌和抗感染效果的传统中药。Oridonin 抑制AKT1 和 AKT2的激酶活性,对应的IC50值分别为8.4μM 和 8.9μM。 |
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靶点 |
Akt1 8.4μM |
Akt2 8.9μM |
体外研究 |
Oridonin有效抑制各种癌细胞的增殖,包括来自前列腺癌 (LNCaP, DU145, PC3),乳腺癌(MCF-7, MDA-MB231),非小细胞肺癌 (NSCL) (NCI-H520, NCI-H460, NCI-H1299),急性早幼粒细胞白血病(NB4),以及胶质母细胞瘤(U118, U138)的细胞增殖,ED50s的范围为1.8 to 7.5 μ克/毫升。Oridonin的抗肿瘤活性可能是由于它对NF-κB和MAPKs信号通路的抑制作用。 |
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体内研究 |
LD50:小鼠35-40毫克/千克。 |
推荐实验方法(仅供参考)
Kinase Assay |
For the AKT kinase assay, the ADP-Glo™ Kinase Assay Kit is used. Active AKT1 or AKT2 kinase and inactive GSK-3β as substrate are mixed by 1× reaction buffer and then added to a white 96-well plate. Pure ATP provided in the kit is serially diluted obtain a final concentration of 0, 1, 10, 50, and 100μM. GSK-3β is added to reach a final concentration of 2.5, 5, 10 or 20μM and DMSO is used as a control. The mixed solution is incubated at room temperature and luciferase activity is measured using the Luminoskan Ascent plate reader |
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Cell Assay |
Cells are seeded (6×103 cells/well for KYSE70; 2.5×103 cells/well for KYSE410; 2×103 cells/well for KYSE450) in 96-well plates and incubated for 24 h and then treated with different amounts of Oridonin or vehicle. After incubation for 24, 48 or 72 h, cell proliferation is measured by the MTT assay. For anchorage-independent cell growth assessment, cells (2.5, 5 or 10μM Oridonin) suspended in complete medium are added to 0.3% agar with vehicle, 2.5, 5 or 10μM Oridonin in a top layer over a base layer of 0.5% agar with vehicle, 2.5, 5 or 10μM Oridonin. The cultures are maintained at 37°C in a 5% CO2 incubator for 3 weeks and then colonies are visualized under a microscope and counted using the Image-Pro Plus software program |
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Animal Administration |
Mice Breast cancer cells are harvested and resuspended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100μL per site) into the fourth pair of mammary fat pads of nude mice (CrTac: NCr-Foxn1nu). Tumors are measured in two dimensions using manual calipers. Tumor volume is calculated using the formula: Volume = 0.5 × length × width × width. Tumor volume is measured every 2-3 days. Upon harvesting, tumors are fixed in formalin overnight and then in 70% ethanol for histopathology analysis. Mice are treated with Oridonin (15mg/kg) in 1% Pluronic F68 or vehicle (1% Pluronic F68) daily by intraperitoneal (IP) injection. BEZ235 is reconstituted 1:9 in 1-methyl-2 pyrolidone and polyethylene glycol 300 (PEG300) Mice are treated with this compound formulation at 45mg/kg daily (QD) by oral gavage |
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 )