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Trabectedin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Trabectedin图片
CAS NO:114899-77-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品名称
曲贝替定
Ecteinascidin 743
ET-743
产品介绍
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。
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 andcancercellsapoptosis, and increases the generation ofROSin MCF-7 and MDA-MB-453 cells. Trabectedin has the potential for soft tissue sarcoma and ovariancancerresearch[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 IC50values 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].

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].

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

性状

Solid

Formula

C39H43N3O11S

CAS 号

114899-77-3

中文名称

他比特啶;他比特定;曲贝替定

结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
来源

marine ascidian

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 mg5 mg10 mg
1 mM1.3126 mL6.5631 mL13.1261 mL
5 mM0.2625 mL1.3126 mL2.6252 mL
10 mM0.1313 mL0.6563 mL1.3126 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-CDin 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 μL20% 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本网站选购。