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) 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.

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3-Fluoro-evodiamine glucose Chemical Structure

3-Fluoro-evodiamine glucose Chemical Structure

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3-Fluoro-evodiamine glucose Related Antibodies

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Description

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

 

In Vitro

3-Fluoro-evodiamine glucose (0-0.5 μM, 12 h) exhibits antiproliferative and cytotoxic property in cancer cells U87MG, A549 and HCT116 with IC50 range of 0.064–0.113 μM, through induction of reactive oxygen species (ROS) accumulation and DNA damage[1].
3-Fluoro-evodiamine glucose (0-0.05 μM, 24 h) inhibits the migration and invasion of cell HCT116 in a dose-dependent manner[1].

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

3-Fluoro-evodiamine glucose Related Antibodies

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%.
In Vivo

3-Fluoro-evodiamine glucose (10 mg/kg, ip, single dose) a good pharmacokinetic property in mice, with a half life of 2.41 h, a plasma concentration Cmax of 4627 h·ng/mL, an AUC0-t of 4008 h·ng/mL and a mean residence time of 0.802 h[1].
3-Fluoro-evodiamine glucose (10-20 mg/kg, ip, twice daily for 21 days) exhibits antitumor efficacy with a tumor growth inhibition TGI of 72%-82% in HCT116 xenograft nude mice, without significant toxicity[1].

MedChemExpress (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.
Molecular Weight

499.49

Formula

C25H26FN3O7
SMILES

O[C@H]1[C@@H]([C@H]([C@@H](O[C@@H]1CO)OC2=CC3=C(NC4=C3CCN5[C@]4([H])N(C6=C(C5=O)C=C(F)C=C6)C)C=C2)O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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3-Fluoro-evodiamine glucose Related Classifications

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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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