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  2. 天然產(chǎn)物
  3. 疾病研究領(lǐng)域 植物 甾體類
  4. 百合科 癌癥
  5. 虎眼萬年青
  6. OSW-1

OSW-1 是從虎眼萬年青中分離出來的，osterol-binding protein (OSBP) 和 OSBP-elated protein 4 (ORP4) 的特異性拮抗劑，其在人類腫瘤細胞系中的 GI50 值為納摩爾級別。

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OSW-1 Chemical Structure

OSW-1 Chemical Structure

CAS No. : 145075-81-6

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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].
細胞效力
(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]
體外研究
(In Vitro)

OSW-1 對結(jié)腸癌細胞有很強的抑制作用，對正常細胞的細胞毒性較低。OSW-1 對 SW480 和 LoVo 結(jié)腸癌細胞的抗增殖作用通過使用 CCK8 測定法測量細胞活力來表征，并將結(jié)果與其他臨床抗癌劑進行比較。SW480 和 LoVo 細胞系來源于杜克斯 B 期結(jié)腸癌和結(jié)腸癌轉(zhuǎn)移性結(jié)節(jié)，分別代表非轉(zhuǎn)移性和轉(zhuǎn)移性癌。OSW-1 不僅在 SW480 和 LoVo 細胞系中表現(xiàn)出極強的抗癌活性，IC50 為納摩爾濃度，而且比其他抗癌藥物的效力高 10-100 倍，細胞毒性更低對正常上皮細胞具有較低的細胞毒性作用。這些結(jié)果表明 OSW-1 具有強大的抗癌作用，但對正常細胞的細胞毒作用較低[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

為了確定 OSW-1 在體內(nèi)是否同樣有效，采用了接種 LoVo 細胞的裸鼠模型，當(dāng)腫瘤變得可觸及時進行 OSW-1 處理。結(jié)果表明，接受處理的小鼠體內(nèi)腫瘤的大小平均小于對照小鼠。從處理后第15-17 天開始觀察到顯著差異，并且這種差異逐漸增加直至處死動物。與對照組相比，OSW-1 處理組的腫瘤重量顯著降低 (P<0.05)。此外，在 OSW-1 處理的小鼠中沒有觀察到明顯的副作用。這些結(jié)果表明 OSW-1 具有強大的抑制結(jié)腸腫瘤生長的作用，并且在體內(nèi)沒有明顯的副作用[2]。

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

873.03

Formula

C47H68O15
CAS 號
性狀

固體

顏色

White to off-white

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

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

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (114.54 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備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儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.86 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.86 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.66%

參考文獻
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.
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備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儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
OSW-1
目錄號：
HY-101213
需求量：