1. PI3K/Akt/mTOR Anti-infection
  2. Akt Bacterial
  3. Oridonin

Oridonin  (Synonyms: 冬凌草甲素; NSC-250682; Isodonol)

目录号: HY-N0004 纯度: 99.89%
COA 产品使用指南

Oridonin (NSC-250682) 是从 Rabdosia rubescens 中得到的二萜,为 AKT 抑制剂,对 AKT1AKT2IC50 值分别为 8.4 和 8.9 μM;Oridonin 具有抗肿瘤、抗菌、抗炎等功效。

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Oridonin Chemical Structure

Oridonin Chemical Structure

CAS No. : 28957-04-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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1 mg ¥156
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5 mg ¥312
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10 mg ¥500
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50 mg ¥1000
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100 mg ¥1600
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200 mg ¥2600
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500 mg ¥5200
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Customer Review

查看 Akt 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.

IC50 & Target[1]

Akt1

8.4 μM (IC50)

Akt2

8.9 μM (IC50)

体外研究
(In Vitro)

Oridonin is an ATP-competitive inhibitor of AKT with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2, respectively. Oridonin (5, 10 or 20 μM) obviously inhibits the growth of KYSE70, KYSE410 and KYSE450 ESCC cells via targeting AKT1/2. Oridonin (10 or 20 μM) causes G2/M phase cell cycle arrest in KYSE70, KYSE410 and KYSE450 cells, and induces apoptosis in these three cell lines at 20 μM. In addition, Oridonin (5, 10 or 20 μM) in combination with cisplatin or 5-FU enhances the inhibition of esophageal squamous cell carcinoma (ESCC) cell growth[1]. Oridonin (0.1 and 1 μM) preferentially suppresses AKT/mTOR signaling. Oridonin (1 μM) also selectively suppresses growth of breast cancer cells with hyperactivation of AKT signaling[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oridonin (160 mg/kg, p.o.) shows significant reduction in the tumor growth without obvious weigh loss in SCID mice bearing EG9 and HEG18 tumor cells. Oridonin treatment also suppresses the expression of Ki-67, phosphorylated AKT, GSK-3β or mTOR in mice[1]. Oridonin (15 mg/kg, i.p.) impairs cell growth in breast cancer with hyperactivation of AKT signaling in nude mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

364.43

Formula

C20H28O6

CAS 号
性状

固体

颜色

White to off-white

中文名称

冬凌草甲素

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 62.5 mg/mL (171.50 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7440 mL 13.7201 mL 27.4401 mL
5 mM 0.5488 mL 2.7440 mL 5.4880 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.71 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.71 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: 10% 1-Methyl-2-pyrrolidinone    90% PEG300

    Solubility: ≥ 5 mg/mL (13.72 mM); 澄清溶液

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.89%

参考文献
Kinase Assay
[1]

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 100 μM. GSK-3β is added to reach a final concentration of 2.5, 5, 10 or 20 μM 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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 10 μM Oridonin) suspended in complete medium are added to 0.3% agar with vehicle, 2.5, 5 or 10 μM Oridonin in a top layer over a base layer of 0.5% agar with vehicle, 2.5, 5 or 10 μM 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]
Breast cancer cells are harvested and resuspended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100 μL 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 (15 mg/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 45 mg/kg daily (QD) by oral gavage[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Oridonin 相关分类

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7440 mL 13.7201 mL 27.4401 mL 68.6003 mL
5 mM 0.5488 mL 2.7440 mL 5.4880 mL 13.7201 mL
10 mM 0.2744 mL 1.3720 mL 2.7440 mL 6.8600 mL
15 mM 0.1829 mL 0.9147 mL 1.8293 mL 4.5734 mL
20 mM 0.1372 mL 0.6860 mL 1.3720 mL 3.4300 mL
25 mM 0.1098 mL 0.5488 mL 1.0976 mL 2.7440 mL
30 mM 0.0915 mL 0.4573 mL 0.9147 mL 2.2867 mL
40 mM 0.0686 mL 0.3430 mL 0.6860 mL 1.7150 mL
50 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3720 mL
60 mM 0.0457 mL 0.2287 mL 0.4573 mL 1.1433 mL
80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8575 mL
100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6860 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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