Ecteinascidin 770 纯度:98.82% 10mM*1mL in DMSO

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Ecteinascidin 770 纯度:98.82% 10mM*1mL in DMSO

市场价：: 141944.00

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货号：HY-101191

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商品介绍
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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。

Description

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]

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].

Solvent & Solubility

In Vitro:

10 mM in DMSO

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

References

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

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

References

[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.

Molecular Weight	770.85
Formula	C₄₀H₄₂N₄O₁₀S
CAS No.	114899-80-8
SMILES	N#C[C@@H]([C@@]1([H])N(C)[C@]2([H])C3=C(C=C(C)C(OC)=C3O)C1)N4[C@@]2([H])[C@@](SC[C@@]5(NCC6)C7=C6C=C(O)C(OC)=C7)([H])C8=C(C(OCO9)=C9C(C)=C8OC(C)=O)[C@]4([H])COC5=O
Storage	4°C, stored under argon
Shipping	Room temperature in continental US; may vary elsewhere