2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage Apoptosis
  3. GLUT Topoisomerase Apoptosis
  4. 3-Fluoro-evodiamine glucose

3-Fluoro-evodiamine glucose (Compound 8) 是一种吴茱萸碱-葡萄糖缀合物。3-Fluoro-evodiamine glucose 激活葡萄糖转运蛋白 1 (GLUT1) 的表达，抑制 topoisomerase I/II 活性。3-Fluoro-evodiamine glucose 诱导细胞凋亡 (apoptosis)，在 G2/M 期阻滞细胞周期。3-Fluoro-evodiamine glucose 在体内和体外均表现出抗肿瘤活性，且无明显毒性。

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3-Fluoro-evodiamine glucose Chemical Structure

3-Fluoro-evodiamine glucose Chemical Structure

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3-Fluoro-evodiamine glucose 相关抗体

Top Publications Citing Use of Products

查看 GLUT 亚型特异性产品:

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GLUT1 GLUT2 GLUT3 GLUT4

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity[1].

IC50 & Target

Topoisomerase I

 

Topoisomerase II

 

GLUT1

 

体外研究
(In Vitro)

3-Fluoro-evodiamine glucose (0-0.5 μM，12 h) 通过诱导活性氧 (ROS) 积累和 DNA 损伤，在癌细胞 U87MG、A549 和 HCT116 中表现出抗增殖活性和细胞毒性，IC50 为 0.064–0.113 μM[1]。
3-Fluoro-evodiamine glucose (0-0.05 μM，24 h) 剂量依赖地抑制 HCT116 细胞的迁移和侵袭[1]。

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

3-Fluoro-evodiamine glucose 相关抗体:

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 0-0.5 μM
Incubation Time: 12 h
Result: Upregulated levels of γ-H2AX and induced DNA damage.

Cell Migration Assay [1]

Cell Line: HCT116
Concentration: 0-0.05 μM
Incubation Time: 24 h
Result: Repressed the wound heal with the rate of 37%-1.1%.
体内研究
(In Vivo)

3-Fluoro-evodiamine glucose (10 mg/kg，腹腔注射，单剂量) 在小鼠体内表现出良好的药代动力学特性，半衰期为 2.41 h，血浆暴露度 Cmax 为 4627 h·ng/ mL，AUC0-t 为 4008 h·ng/mL，平均停留时间为 0.802 h[1]。
3-Fluoro-evodiamine glucose (10-20 mg/kg，腹腔注射，每天两次，持续 21 天) 在 HCT116 异种移植裸鼠中表现出抗肿瘤功效，肿瘤生长抑制率 TGI 为 72%-82%，且无明显毒性[1]。

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

Animal Model: HCT116 xenograft BALB/c nude mice[1]
Dosage: 10-20 mg/kg
Administration: ip, two injections every days for 21 days
Result: Inhibited tumor growth with TGI of 72-82%, without body weight loss.
分子量

499.49

Formula

C25H26FN3O7
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

3-Fluoro-evodiamine glucose 相关分类

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  • 稀释计算器

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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.

Keywords:

3-Fluoro-evodiamine glucoseGLUTTopoisomeraseApoptosisGlucose transporter U87MGA549HCT116astroblastomacolon cancerlung cancerBALB/c miceInhibitorinhibitorinhibit

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