Ecteinascidin-Analog-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ecteinascidin-Analog-1 

Ecteinascidin-Analog-1是海鞘素类似物化学合成中的中间体,海鞘素是一类具有光谱抗癌和抗感染活性的四氢异喹啉类生物碱。

Ecteinascidin-Analog-1

Ecteinascidin-Analog-1 Chemical Structure

CAS No. : 874758-58-4

规格 价格 是否有货
2 mg ¥2333 询问价格 & 货期
5 mg ¥3500 询问价格 & 货期
10 mg ¥5000 询问价格 & 货期

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生物活性

Ecteinascidin-Analog-1 is a useful intermediate for chemical sythesis of Ecteinascidin analogues; Ecteinascidins is a family of tetrahydroisoquinoline alkaloids with wide range of antitumor and antimicrobial activities.

分子量

588.69

Formula

C31H44N2O9

CAS 号

874758-58-4

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 6 months
-20°C 1 month
参考文献
  • [1]. Chen J, et al. Asymmetric total syntheses of ecteinascidin 597 and ecteinascidin 583. Angew Chem Int Ed Engl. 2006 Dec 4;45(47):8028-32.

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Ecteinascidin 770(Synonyms: Ecteinascidine 770; Et-770)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Ecteinascidin 770 (Synonyms: Ecteinascidine 770; Et-770) 纯度: ≥99.0%

Ecteinascidin 770 (ET-770)是具有抗癌活性的1,2,3,4-四氢异喹啉生物碱,抑制U373MG cells的IC50值为4.83 nM。

Ecteinascidin 770(Synonyms: Ecteinascidine 770;  Et-770)

Ecteinascidin 770 Chemical Structure

CAS No. : 114899-80-8

规格 价格 是否有货 数量
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10 mg ¥4000 In-stock
50 mg ¥12000 In-stock
100 mg   询价  
200 mg   询价  

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Ecteinascidin 770 相关产品

相关化合物库:

  • Natural Product Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Natural Product Library
  • Anti-Cancer Compound Library
  • Phenols Library
  • Alkaloids Library
  • Anti-Lung Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Microbial Metabolite Library

生物活性

Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.

IC50 & Target

IC50: 4.83 nM (U373MG cell)[1]; 0.6 nM (HCT116 cell), 2.4 nM (QG56 cell), 0.81 nM (DU145)[2]

体外研究
(In Vitro)

Ecteinascidin 770 induces apoptosis of U373MG cells. The IC50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment[1]. The IC50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively[2]. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

770.85

Formula

C40H42N4O10S

CAS 号

114899-80-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light

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

溶解性数据
In Vitro: 

DMSO : 50 mg/mL (64.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2973 mL 6.4863 mL 12.9727 mL
5 mM 0.2595 mL 1.2973 mL 2.5945 mL
10 mM 0.1297 mL 0.6486 mL 1.2973 mL

*

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)。-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。

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

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (3.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.24 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Tabunoki H, et al. Molecular network profiling of U373MG human glioblastoma cells following induction of apoptosis by novel marine-derived anti-cancer 1,2,3,4-tetrahydroisoquinoline alkaloids. Cancer Cell Int. 2012 Apr 11;12(1):14.

    [2]. Saktrakulkla P, et al. Chemistry of ecteinascidins. Part 3: preparation of 2′-N-acyl derivatives of ecteinascidin 770 and evaluation of cytotoxicity. Bioorg Med Chem. 2011 Aug 1;19(15):4421-36.

    [3]. Powan P, et al. Ecteinascidin 770, a tetrahydroisoquinoline alkaloid, sensitizes human lung cancer cells to anoikis. Anticancer Res. 2013 Feb;33(2):505-12.

Cell Assay
[3]

Ecteinascidin 770 is dissolved in DMSO and diluted with appropriate medium. H23 and H460 cells are seeded into 96-well plates at 1×105 cell/mL for 24 h and then treated with different concentrations of ecteinascidin 770 for 24 h. Cells are then incubated with 20 μM of XTT reagent for a further 4 h at 37°C. The intensity of the formazan product is measured at 450 nm using a microplate reader. The cell viability is calculated from the optical density (OD) ratio of treated to non-treated control cells and is presented as a percentage to that of the non-treated controls[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Tabunoki H, et al. Molecular network profiling of U373MG human glioblastoma cells following induction of apoptosis by novel marine-derived anti-cancer 1,2,3,4-tetrahydroisoquinoline alkaloids. Cancer Cell Int. 2012 Apr 11;12(1):14.

    [2]. Saktrakulkla P, et al. Chemistry of ecteinascidins. Part 3: preparation of 2′-N-acyl derivatives of ecteinascidin 770 and evaluation of cytotoxicity. Bioorg Med Chem. 2011 Aug 1;19(15):4421-36.

    [3]. Powan P, et al. Ecteinascidin 770, a tetrahydroisoquinoline alkaloid, sensitizes human lung cancer cells to anoikis. Anticancer Res. 2013 Feb;33(2):505-12.

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Trabectedin(Synonyms: 曲贝替定; Ecteinascidin 743; ET-743)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Trabectedin (Synonyms: 曲贝替定; Ecteinascidin 743; ET-743) 纯度: 99.82%

Trabectedin (Ecteinascidin 743; ET-743) 是一种四氢异喹啉生物碱,具有有效的抗肿瘤活性。 Trabectedin 与 DNA 的小沟结合,阻断应激诱导的蛋白质的转录,诱导 DNA 骨架裂解和癌细胞凋亡 (apoptosis),并增加 MCF-7 和 MDA-MB-453 细胞中 ROS 的生成。Trabectedin 可用于软组织肉瘤和卵巢癌的研究。

Trabectedin(Synonyms: 曲贝替定; Ecteinascidin 743;  ET-743)

Trabectedin Chemical Structure

CAS No. : 114899-77-3

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1 mg ¥3200 In-stock
5 mg ¥9800 In-stock
10 mg   询价  
50 mg   询价  

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  • Natural Product Library Plus
  • Drug Repurposing Compound Library Plus
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生物活性

Trabectedin (Ecteinascidin 743; ET-743) is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has the potential for soft tissue sarcoma and ovarian cancer research[1][2][3].

IC50 & Target

IC50: 0.1 nM (MX-1 cells), 1.5 nM (MCF7 cells) and 3.7 nM (MCF7/DXR cells)[1]
Reactive oxygen species (ROS)[2]
Apoptosis[2]

体外研究
(In Vitro)

Trabectedin (ET-743; 10 nM; 24-72 hours; MCF7 cells) treatment results in cell accumulation in late S to G2 phase[1].
Trabectedin inhibits cell growth of MX-1, MCF7 and MCF7/DXR cells with IC50 values of 0.1 nM, 1.5 nM and 3.7 nM, respectively[1].
Trabectedin induces cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. The expression levels of the death receptor pathway molecules, TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD are significantly increased by 2.6-, 3.1-, 1.7-, 11.2- and 4.0-fold by Trabectedin treatment in MCF-7 cells. In MDA-MB-453 cells, the mitochondrial pathway related pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and Cleaved Caspase-3 expressions are induced by 4.2-, 3.6-, 4.8-, 4.5-, and 4.4-fold, and the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-XL are reduced by 4.8- and 5.2-fold in MDA-MB-453 cells[2].
In vitro treatment with noncytotoxic concentrations of Trabectedin selectively inhibits the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by myxoid liposarcoma (MLS) primary tumor cultures and/or cell lines[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MCF7 cells
Concentration: 10 nM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Led to pronounced S-G2-M accumulation.

体内研究
(In Vivo)

Trabectedin (ET-743; 30-50 μg/kg; intravenous injection; every three days; female athymic nude mice) treatment increases the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity[1].
A xenograft mouse model of human myxoid liposarcoma (MLS) shows marked reduction of CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decrease of PTX3 after Trabectedin treatment[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice bearing the nu/nu gene (5-6 weeks old, 18-20 g) injected with MX-1 cells[1]
Dosage: 30 μg/kg, 40 μg/kg, 50 μg/kg
Administration: Intravenous injection; every three days
Result: Increased the antitumor effects in nude mice bearing MX-1 mammary carcinoma xenografts without increasing toxicity.

Clinical Trial

分子量

761.84

Formula

C39H43N3O11S

CAS 号

114899-77-3

中文名称

他比特啶;他比特定;曲贝替定

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (43.75 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3126 mL 6.5631 mL 13.1261 mL
5 mM 0.2625 mL 1.3126 mL 2.6252 mL
10 mM 0.1313 mL 0.6563 mL 1.3126 mL

*

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

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

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.28 mM,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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.28 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

  • 3.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (3.28 mM); Clear solution

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Takahashi N, et al. Sequence-dependent synergistic cytotoxicity of ecteinascidin-743 and NSC 125973 in human breast cancer cell linesin vitro and in vivo. Cancer Res. 2002 Dec 1;62(23):6909-15.

    [2]. Atmaca H, et al. A diverse induction of apoptosis by trabectedin in MCF-7 (HER2-/ER+) and MDA-MB-453 (HER2+/ER-) breast cancer cells. Toxicol Lett. 2013 Jun 20;221(2):128-136.

    [3]. Germano G, et al. Antitumor and anti-inflammatory effects of trabectedin on human myxoid liposarcoma cells. Cancer Res. 2010 Mar 15;70(6):2235-44.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务