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  2. Apoptosis Anti-infection Membrane Transporter/Ion Channel Neuronal Signaling
  3. Bcl-2 Family Caspase Apoptosis HSV Na+/K+ ATPase Calcium Channel
  4. Digitoxin

Digitoxin  (Synonyms: 洋地黃毒苷)

目錄號: HY-B1357 純度: 99.36%
COA 產(chǎn)品使用指南

Digitoxin 是一種抗癌劑。Digitoxin 可誘導細胞凋亡 (apoptosis)、抑制流感細胞因子風暴、引起 DNA 雙鏈斷裂(DSBs)、將細胞周期阻滯在 G2/M 期。Digitoxin 通過形成跨膜鈣通道誘導細胞內(nèi)鈣攝取，可用于心力衰竭的研究。

MCE 的所有產(chǎn)品僅用作科學研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務

Digitoxin Chemical Structure

Digitoxin Chemical Structure

CAS No. : 71-63-6

1.  客戶無需承擔相應的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥673
In-stock
5 mg ￥500
In-stock
10 mg ￥800
In-stock
50 mg ￥2400
In-stock
100 mg ￥3600
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Digitoxin:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure [1][2][3][4][5].

IC50 & Target

Bcl-2

 

Caspase-9

 

Caspase 3

 

Bax

 

HSV-1

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay
Cytotoxicity against human A549 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
Cancer cell lines IC50
0.1 μM
Compound: 2
Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
Cytotoxicity against human colon cancer cells after 72 hrs by FMCA method
[PMID: 19894733]
DU-145 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay
Cytotoxicity against human DU145 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
HCT-116 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay
Cytotoxicity against human HCT116 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
HCT-116 IC50
0.74 μM
Compound: 2
Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
Cytotoxicity against human HCT116 cells after 72 hrs by FMCA method
[PMID: 19894733]
Hep 3B2 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay
Cytotoxicity against human Hep3B cells after 72 hrs by calcein AM assay
[PMID: 16309329]
HFF CC50
2.8 μM
Compound: 1
Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay
Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by MTT assay
[PMID: 24900847]
HFF CC50
6 μM
Compound: 1
Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay
Cytotoxicity against HFF assessed as inhibition of cell viability after 3 days by trypan blue exclusion assay
[PMID: 24900847]
HT-29 IC50
0.068 μM
Compound: (+)-Digitoxin
Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human HT-29 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
HT-29 IC50
4.07 μM
Compound: 2
Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
Cytotoxicity against human HT-29 cells after 72 hrs by FMCA method
[PMID: 19894733]
HT-29 IC50
67.6 nM
Compound: Digitoxin
Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human HT-29 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
K562 IC50
6.4 nM
Compound: 1
Cytotoxicity against human K562 cells by XTT assay
Cytotoxicity against human K562 cells by XTT assay
[PMID: 16309315]
KURAMOCHI IC50
5911 nM
Compound: Digitoxin
Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human Kuramochi cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
MCF7 IC50
0.02 μM
Compound: 1, DT
Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay
Antiproliferative activity against human MCF7 cells assessed as cell viability treated for 48 hrs followed by compound washout measured after 72 hrs by fluorometric CellTiter-Blue reagent assay
[PMID: 21421322]
MCF7 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
MCF7 IC50
10.2 nM
Compound: 1
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 16309315]
MDA-MB-231 IC50
0.48 μM
Compound: (+)-Digitoxin
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
MDA-MB-231 IC50
482 nM
Compound: Digitoxin
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
MDA-MB-435 IC50
0.043 μM
Compound: (+)-Digitoxin
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
MDA-MB-435 IC50
43.3 nM
Compound: Digitoxin
Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MDA-MB-435 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
NCI/ADR-RES IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay
Cytotoxicity against human NCI/ADR-RES cells after 72 hrs by calcein AM assay
[PMID: 16309329]
NCI-H460 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay
Cytotoxicity against human NCI-H460 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
NCI-H460 GI50
10.7 nM
Compound: 1
Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay
Growth inhibition of human NCI-H460 cells after 48 hrs by MTT assay
[PMID: 21643465]
NCI-H460 IC50
357 nM
Compound: 1
Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining
Cytotoxicity against human NCI-H460 cells assessed as cell death at 50 nM after 12 hrs by Hoechst-33342 staining and propidium iodide staining
[PMID: 21643465]
OVCAR-3 IC50
0.12 μM
Compound: (+)-Digitoxin
Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
Cytotoxicity against human OVCAR3 cells after 72 hrs by CellTiter 96 Aqueous One Solution reagent based assay
[PMID: 32096998]
OVCAR-3 IC50
117.1 nM
Compound: Digitoxin
Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human OVCAR3 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
OVCAR-4 IC50
425.6 nM
Compound: Digitoxin
Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human OVCAR4 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
OVCAR-5 IC50
321 nM
Compound: Digitoxin
Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human OVCAR5 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
OVCAR-8 IC50
71.5 nM
Compound: Digitoxin
Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human OVCAR8 cells after 72 hrs by CellTiter 96 aqueous one solution assay
[PMID: 28234008]
SF-268 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay
Cytotoxicity against human SF268 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
SK-OV-3 IC50
0.44 μM
Compound: digitoxin
Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay
Cytotoxicity against human SKOV3 cells after 72 hrs by calcein AM assay
[PMID: 16309329]
TK-10 IC50
3.2 nM
Compound: 1
Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
Cytotoxicity against human TK10 cells after 48 hrs by SRB assay
[PMID: 16309315]
UACC-62 IC50
33.5 nM
Compound: 1
Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay
[PMID: 16309315]
Vero IC50
< 0.23 μM
Compound: Digitoxin
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
Vero CC50
> 50 μM
Compound: Digitoxin
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
體外研究
(In Vitro)

Digitoxin (0-80 nM, 72 h) 降低 PC12 細胞的存活率[1]。
Digitoxin (4-1000 nM, 24-48 h) 在 MHCC97H, A549, HCT116 和 HeLa 細胞中具有抗腫瘤作用[3]。
Digitoxin (4-100 nM, 24-48 h) 干擾 HeLa 細胞的細胞周期[3]。
Digitoxin (20-500 nM, 48 h) 激活 HeLa 細胞線粒體凋亡[3]。

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

Cell Viability Assay[3]

Cell Line: MHCC97H, A549, HCT116 and HeLa cells
Concentration: 4-1000 nM
Incubation Time: 24 h, 48 h
Result: Dcreased the viability of these cancer cells in a dose- and time-dependent manner, with the IC50 values ranging from 0.075 to 0.395 μM following digitoxin treatment for 24 h and from 0.028 to 0.077 μM following digitoxin treatment for 48 h.

Cell Cycle Analysis[3]

Cell Line: HeLa cells
Concentration: 4 nM, 20 nM, 100 nM
Incubation Time: 24 h, 36 h, 48 h
Result: Increased cell population in the G2/M phase from 16.27 to 18.36, 23.46 and 31.51% at concentrations of 20 nM for12, 24 and 36 h.
Increased average cell population in the G2/M phase from 16.27 to 28.07% at concentrations of 4, 20 and 100 nM for 24 h.
Significantly decreased the protein expression levels of total CDK1 and phosphorylated CDK1.

Apoptosis Analysis[3]

Cell Line: HeLa cells
Concentration: 20 nM, 100 nM, 500 nM
Incubation Time: 48 h
Result: Upregulated Bax expression and unaltered Bcl-2 expression.
Significantly increased the expression of cytochrome c.
體內(nèi)研究
(In Vivo)

Digitoxin (1-2 mg/kg, Intraperitoneal injection, once a day for 19 days) 在裸鼠中具有抗癌作用[3]。
Digitoxin (0.3-3 μg/kg, Intraperitoneal injection, once a day for 4 days) 阻斷棉花鼠肺內(nèi)宿主細胞因子的過度產(chǎn)生[4]。

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

Animal Model: nude mice harboring HeLa tumor xenografts[3]
Dosage: 1 mg/kg, 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Decreased the tumor volume from 330.71±45.61 to 214.56.93±73.25 mm.
Strongly increased the protein levels of cleaved caspase-3.
Reduced the number of Ki-67-positive cells.
Animal Model: cotton rats[4]
Dosage: 0.3 μg/kg, 1 μg/kg, 3 μg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Blocked cytokine storm.
Differentially affected cytokine expression.
Left immune cell density intact in virus-infected lung.
Clinical Trial
分子量

764.94

Formula

C41H64O13
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

地高辛EP雜質(zhì)A)
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (130.73 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 1.3073 mL 6.5365 mL 13.0729 mL
5 mM 0.2615 mL 1.3073 mL 2.6146 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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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?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，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
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 (3.27 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 (3.27 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）。
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: 99.36%

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，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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 1.3073 mL 6.5365 mL 13.0729 mL 32.6823 mL
5 mM 0.2615 mL 1.3073 mL 2.6146 mL 6.5365 mL
10 mM 0.1307 mL 0.6536 mL 1.3073 mL 3.2682 mL
15 mM 0.0872 mL 0.4358 mL 0.8715 mL 2.1788 mL
20 mM 0.0654 mL 0.3268 mL 0.6536 mL 1.6341 mL
25 mM 0.0523 mL 0.2615 mL 0.5229 mL 1.3073 mL
30 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0894 mL
40 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8171 mL
50 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6536 mL
60 mM 0.0218 mL 0.1089 mL 0.2179 mL 0.5447 mL
80 mM 0.0163 mL 0.0817 mL 0.1634 mL 0.4085 mL
100 mM 0.0131 mL 0.0654 mL 0.1307 mL 0.3268 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：
Digitoxin
目錄號：
HY-B1357
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