1. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Apoptosis Bcl-2 Family Survivin Reactive Oxygen Species (ROS)
  3. Entadamide A-CO-C12

Entadamide A-CO-C12 是 Entadamide A (HY-N12125) 的衍生物,具有强效的抗癌活性,尤其对乳腺癌细胞系有效。Entadamide A-CO-C12 可促进细胞凋亡 (apoptosis),抑制细胞迁移能力、球体形成和干细胞样细胞群。Entadamide A-CO-C12 可抑制 4T1 小鼠模型中的肿瘤生长。Entadamide A-CO-C12 可用于乳腺癌的研究。

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Entadamide A-CO-C12

Entadamide A-CO-C12 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer[1].

体外研究
(In Vitro)

Entadamide A-CO-C12 (compound 3u) (48 小时) 对一系列人类癌细胞 (MDA MB-231、DU-145、MCF-7、4T1、NCI-H460、HepG2 和 HEK-293) 表现出抗增殖活性,IC50 分别为 19.11、3.04、2.82、3.26、20.98、18.89 和 77.69 μM,对乳腺癌细胞 (MCF-7 和 4T1) 表现出选择性抗癌活性[1]
Entadamide A-CO-C12 (1.5-3 μM;48 小时-5 天) 抑制 MCF-7 细胞的迁移并下调 EMT 相关转录因子[1]
Entadamide A-CO-C12 (1.5-3 μM;7 天) 抑制球状体形成并降低 MCF-7 细胞的癌干细胞特性[1]。 Entadamide A-CO-C12 (1.5-3 μM;24-48 小时) 通过调节 MCF-7 细胞中抗凋亡 (BCL-2survivin) 和促凋亡 (BAX) 调节因子在转录和翻译水平上的平衡来促进细胞凋亡,并触发线粒体去极化和内在凋亡途径的激活[1]
Entadamide A-CO-C12 (1.5-3 μM;8-24 小时) 可剂量依赖性诱导 MCF-7 细胞中 ROS 产生的显著升高[1]
Entadamide A-CO-C12 (1.5-3 μM;48 小时) 可降低 CD90 和 CD133 水平,造成 DNA 损伤,并以剂量​​依赖的方式触发 MCF-7 细胞的凋亡性核浓缩[1]
Entadamide A-CO-C12 (1.5-3 μM;48 小时) 通过调节 MCF-7 细胞中 ABCG2 介导的外排途径增强 Doxorubicin (HY-15142A) 的敏感性[1]
Entadamide A-CO-C12 与 ABCB1/ABCG2 和 BMI1 存在部分相互作用,有助于调节耐药性和干性[1]

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

Cell Migration Assay [1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 0, 3, 5 days
Result: Markedly reduced cellmigration compared to the untreated control.

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 24 h
Result: Elicited a marked, concentration-dependent increase in apoptosis.
Induced 10% and 42% early apoptosis at 1.5 and 3 μM, respectively.

Real Time qPCR[1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 48 h
Result: Downregulated anti-apoptotic genes survivin, BCL-2 and upregulated pro-apoptotic genes BAX.
Demonstrated significant downregulation of the EMT-promoting transcription factors SLUG and ZEB1.
Revealed a marked downregulation of BMI1 levels.
Markedly downregulated mRNA expression of ABCG2, ABCC1, and ABCB1.
体内研究
(In Vivo)

Entadamide A-CO-C12 (30 mg/kg,腹腔注射,每天一次,持续 15 天,从第 7 天开始) 在 4T1 原位乳腺癌小鼠模型中表现出强效的体内抗癌活性,且无系统毒性[1]

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

Animal Model: Female-BALB/c mice (6-8 weeks old) subcutaneously injected with 4T1 murine mammary carcinoma cells[1]
Dosage: 30 mg/kg
Administration: i.p., daily for 15 days from day7
Result: Significantly inhibited tumor progression compared to control.
Showed significant size reductions relative to controls.
Showed no significant body weight changes or systemic toxicity.
分子量

357.55

Formula

C19H35NO3S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

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)
× = ×
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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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产品名称:
Entadamide A-CO-C12
目录号:
HY-179615
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