Echinomycin(Synonyms: Quinomycin A; NSC-13502)

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Echinomycin (Synonyms: Quinomycin A; NSC-13502) 纯度: ≥98.0%

Echinomycin (Quinomycin A) 是一种有效的,细胞渗透性的低氧诱导因子-1 (HIF-1) DNA 结合活性的小分子抑制剂。Echinomycin 选择性抑制癌症干细胞，其 IC50 值为 29.4 pM。

Echinomycin(Synonyms: Quinomycin A; NSC-13502)

Echinomycin Chemical Structure

CAS No. : 512-64-1

规格 价格 是否有货 数量
1 mg ￥3600 In-stock
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10 mg   询价  

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生物活性

Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM[1][2].

体外研究
(In Vitro)

Echinomycin (0-10 nM; 16 hours; U251 cells) treatment significantly inhibits hypoxia-induced VEGF mRNA expression in a dose-dependent fashion. Echinomycin very potently inhibits hypoxic induction of luciferase expression in U251-HRE in a dose-dependent fashion with an EC50 of 1.2 nM[1].

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.

RT-PCR[1]

Cell Line: U251 cells
Concentration: 0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM
Incubation Time: 16 hours
Result: Significantly inhibited VEGF mRNA expression induced by hypoxia in a dose-dependent fashion.

体内研究
(In Vivo)

Echinomycin (10 μg/kg; intravenous injection; for 40 days; NOD-SCID mice) treatment efficiently eradicates mouse lymphoma and serially transplantable human acute myeloid leukemia (AML) in xenogeneic model by preferential elimination of cancer stem cells (CSCs). HIF1α maintains mouse lymphoma CSCs by repressing a negative feedback loop in the Notch pathway[2].

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: NOD-SCID mice received 1.8Gy of irradiation and i.v. injection with peripheral blood cells from patients AML-71 and AML-150[2]
Dosage: 10 μg/kg
Administration: Intravenous injection; for 40 days
Result: Efficiently eradicated mouse lymphoma and serially transplantable human AML in xenogeneic model by preferential elimination of CSCs.

分子量

1101.26

Formula

C51H64N12O12S2
CAS 号

512-64-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶解性数据
In Vitro: 

DMSO : 5.3 mg/mL (4.81 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9081 mL 4.5403 mL 9.0805 mL
5 mM — — —
10 mM — — —

*

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 (stored under nitrogen)。-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。
参考文献

  • [1]. Kong D, et al. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res. 2005 Oct 1;65(19):9047-55.

    [2]. Wang Y, et al. Targeting HIF1α eliminates cancer stem cells in hematological malignancies. Cell Stem Cell. 2011 Apr 8;8(4):399-411.

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