1. 天然产物
  2. 疾病研究领域 植物 甾体类
  3. 百合科 癌症
  4. 虎眼万年青
  5. OSW-1

OSW-1 是从虎眼万年青中分离出来的,osterol-binding protein (OSBP)OSBP-elated protein 4 (ORP4) 的特异性拮抗剂,其在人类肿瘤细胞系中的 GI50 值为纳摩尔级别。

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OSW-1 Chemical Structure

OSW-1 Chemical Structure

CAS No. : 145075-81-6

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MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.

IC50 & Target

OSBP/ORP4[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
27 nM
Compound: OSW-1
Cytotoxicity against human A549 cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human A549 cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
BJ IC50
0.2 nM
Compound: OSW-1
Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
CCRF-CEM IC50
0.3 nM
Compound: OSW-1
Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
G-361 IC50
1000 nM
Compound: OSW-1
Cytotoxicity against human G361 cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human G361 cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
HCT-116 IC50
8400 nM
Compound: OSW-1
Cytotoxicity against human HCT116 assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human HCT116 assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
HeLa IC50
2.6 nM
Compound: 1, OSW-1
Cytotoxicity against human HeLa cells after 24 hrs by XTT assay
Cytotoxicity against human HeLa cells after 24 hrs by XTT assay
[PMID: 24613377]
HeLa IC50
3.4 nM
Compound: OSW-1
Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
HL-60 IC50
0.00025 μM
Compound: 3
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 11170674]
HOS IC50
8200 nM
Compound: OSW-1
Cytotoxicity against human HOS cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human HOS cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
Ishikawa IC50
3 μM
Compound: 5f (OSW-1)
Inhibition of the necrosis induced by compound in endometrial cancer ishikawa cell line after 24 hr
Inhibition of the necrosis induced by compound in endometrial cancer ishikawa cell line after 24 hr
[PMID: 15149699]
MCF7 IC50
2.4 nM
Compound: OSW-1
Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
MCF7 IC50
7 μM
Compound: 5f (OSW-1)
Inhibition of the necrosis induced by compound in breast cancer MCF-7 cell line
Inhibition of the necrosis induced by compound in breast cancer MCF-7 cell line
[PMID: 15149699]
MDA-MB-231 IC50
0.5 μM
Compound: 5f (OSW-1)
Inhibition of the necrosis induced by compound in breast cancer MDAMB-231 cell line
Inhibition of the necrosis induced by compound in breast cancer MDAMB-231 cell line
[PMID: 15149699]
T98 IC50
70 nM
Compound: OSW-1
Cytotoxicity against human T98 cells assessed as viable cells after 72 hrs by calcein AM assay
Cytotoxicity against human T98 cells assessed as viable cells after 72 hrs by calcein AM assay
[PMID: 21438635]
体外研究
(In Vitro)

OSW-1 对结肠癌细胞有很强的抑制作用,对正常细胞的细胞毒性较低。OSW-1 对 SW480 和 LoVo 结肠癌细胞的抗增殖作用通过使用 CCK8 测定法测量细胞活力来表征,并将结果与其他临床抗癌剂进行比较。SW480 和 LoVo 细胞系来源于杜克斯 B 期结肠癌和结肠癌转移性结节,分别代表非转移性和转移性癌。OSW-1 不仅在 SW480 和 LoVo 细胞系中表现出极强的抗癌活性,IC50 为纳摩尔浓度,而且比其他抗癌药物的效力高 10-100 倍,细胞毒性更低对正常上皮细胞具有较低的细胞毒性作用。这些结果表明 OSW-1 具有强大的抗癌作用,但对正常细胞的细胞毒作用较低[2]

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

体内研究
(In Vivo)

为了确定 OSW-1 在体内是否同样有效,采用了接种 LoVo 细胞的裸鼠模型,当肿瘤变得可触及时进行 OSW-1 处理。结果表明,接受处理的小鼠体内肿瘤的大小平均小于对照小鼠。从处理后第15-17 天开始观察到显著差异,并且这种差异逐渐增加直至处死动物。与对照组相比,OSW-1 处理组的肿瘤重量显著降低 (P<0.05)。此外,在 OSW-1 处理的小鼠中没有观察到明显的副作用。这些结果表明 OSW-1 具有强大的抑制结肠肿瘤生长的作用,并且在体内没有明显的副作用[2]

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

分子量

873.03

Formula

C47H68O15

CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (114.54 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 1.1454 mL 5.7272 mL 11.4544 mL
5 mM 0.2291 mL 1.1454 mL 2.2909 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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

动物实验:

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: ≥ 2.5 mg/mL (2.86 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (2.86 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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。

    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。
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)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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: 99.66%

参考文献
Cell Assay
[2]

To observe the effect of OSW-1 on cell viability, the colon cancer cell lines LoVo and SW480 cells are seeded in 96-well plates at a concentration of 1×105 cells/well. Following overnight incubation, the cells are treated with several concentrations of OSW-1 (11.25, 22.5, 45, 90, 180 ng/mL) and incubated at 37°C in 5% CO2 for 24, 48, and 72 h. Cell viability analysis is determined using a Cell Counting Kit-8 Assay. Each assay is performed in quintuplicate and repeated three times[2].

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

Animal Administration
[2]

Mice[2]
Four-week-old male nude mice are used. Animals are acclimatized to the animal housing facility for a period of 7 days before the beginning of the experiments. LoVo human colon cancer cells (5x106 cells in 100 μL) are injected subcutaneously into the right flank of 18 nude mice. When the tumor becomes palpable, the nude mice are randomized into two groups: i) intraperitoneal injection of PBS (500 μL) daily in 9 nude mice; and ii) intraperitoneal injection of OSW-1 (0.01 mg/kg diluted in PBS in 500 μL) daily in 9 nude mice. The body weights of the animals and tumor size are recorded every day, and the tumor volume is calculated[2].

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

参考文献

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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1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 1.1454 mL 5.7272 mL 11.4544 mL 28.6359 mL
5 mM 0.2291 mL 1.1454 mL 2.2909 mL 5.7272 mL
10 mM 0.1145 mL 0.5727 mL 1.1454 mL 2.8636 mL
15 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9091 mL
20 mM 0.0573 mL 0.2864 mL 0.5727 mL 1.4318 mL
25 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1454 mL
30 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
40 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7159 mL
50 mM 0.0229 mL 0.1145 mL 0.2291 mL 0.5727 mL
60 mM 0.0191 mL 0.0955 mL 0.1909 mL 0.4773 mL
80 mM 0.0143 mL 0.0716 mL 0.1432 mL 0.3579 mL
100 mM 0.0115 mL 0.0573 mL 0.1145 mL 0.2864 mL
Help & FAQs
  • 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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OSW-1
目录号:
HY-101213
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