Digitoxin (Synonyms: 洋地黄毒苷)

目录号: HY-B1357 纯度: 99.36%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Digitoxin 是一种抗癌剂。Digitoxin 可诱导细胞凋亡 (apoptosis)、抑制流感细胞因子风暴、引起 DNA 双链断裂(DSBs)、将细胞周期阻滞在 G2/M 期。Digitoxin 通过形成跨膜钙通道诱导细胞内钙摄取，可用于心力衰竭的研究。

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Digitoxin Chemical Structure

CAS No. : 71-63-6

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规格	价格	是否有货
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		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Digitoxin:

MCE 顾客使用本产品发表的 6 篇科研文献

Digitoxin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

查看 Caspase 亚型特异性产品:

查看所有亚型

Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 HSV 亚型特异性产品:

查看所有亚型

HSV-1 HSV-2 HSV

查看 Calcium Channel 亚型特异性产品:

查看所有亚型

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

生物活性
纯度 & 产品资料
参考文献

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

细胞效力
(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

体外研究
(In Vitro)

Digitoxin (0-80 nM, 72 h) 降低 PC12 细胞的存活率^[1]。
Digitoxin (4-1000 nM, 24-48 h) 在 MHCC97H, A549, HCT116 和 HeLa 细胞中具有抗肿瘤作用^[3]。
Digitoxin (4-100 nM, 24-48 h) 干扰 HeLa 细胞的细胞周期^[3]。
Digitoxin (20-500 nM, 48 h) 激活 HeLa 细胞线粒体凋亡^[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.

体内研究
(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) 阻断棉花鼠肺内宿主细胞因子的过度产生^[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 号

71-63-6

性状

固体

颜色

White to off-white

中文名称

地高辛EP杂质A)

结构分类

Steroids

初始来源

微生物

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (130.73 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	1.3073 mL	6.5365 mL	13.0729 mL
5 mM	0.2615 mL	1.3073 mL	2.6146 mL
10 mM	0.1307 mL	0.6536 mL	1.3073 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 (3.27 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。
以 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 (3.27 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。
以 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.27 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，此方案实验周期在半个月以上的动物实验酌情使用。
以 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玉米油中，混合均匀。

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

每只动物的给药体积

μL

动物数量

只

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: 99.36%

选择批次：

Data Sheet (642 KB) SDS (644 KB)

COA (288 KB) HNMR (329 KB) LCMS (253 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Arispe N, et al. Heart failure drug digitoxin induces calcium uptake into cells by forming transmembrane calcium channels [J]. Proceedings of the National Academy of Sciences, 2008, 105(7): 2610-2615. [Content Brief]

[2]. Su C T, Hsu J T A, Hsieh H P, et al. Anti-HSV activity of digitoxin and its possible mechanisms [J]. Antiviral research, 2008, 79(1): 62-70.

[3]. Gan H, Qi M, Chan C, et al. Digitoxin inhibits HeLa cell growth through the induction of G2/M cell cycle arrest and apoptosis in vitro and in vivo [J]. International Journal of Oncology, 2020, 57(2): 562-573.

[4]. Pollard B S, Blanco J C, Pollard J R. Classical drug digitoxin inhibits influenza cytokine storm, with implications for COVID-19 therapy [J]. in vivo, 2020, 34(6): 3723-3730.

[5]. Haux J. Digitoxin is a potential anticancer agent for several types of cancer [J]. Medical hypotheses, 1999, 53(6): 543-548.

Digitoxin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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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Digitoxin (Synonyms: 洋地黄毒苷)

Customer Review

Other Forms of Digitoxin:

MCE 顾客使用本产品发表的 6 篇科研文献

Digitoxin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Bcl-2 Family 亚型特异性产品:

查看 Caspase 亚型特异性产品:

查看 HSV 亚型特异性产品:

查看 Calcium Channel 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Digitoxin 相关分类

完整储备液配制表

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Digitoxin (Synonyms: 洋地黄毒苷)

Customer Review

Other Forms of Digitoxin:

Digitoxin 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

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生物活性

纯度 & 产品资料

参考文献

Digitoxin 相关抗体:

摩尔计算器

稀释计算器

Digitoxin 相关分类

完整储备液配制表

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