2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. VEGFR Microtubule/Tubulin Apoptosis
  4. VEGFR-2-IN-71

VEGFR-2-IN-71 is a dual VEGFR2/tubulin inhibitor. VEGFR-2-IN-71 inhibits tumor cell proliferation and induces apoptosis and cell cycle arrest. VEGFR-2-IN-71 inhibits angiogenesis in the chick chorioallantoic membrane (CAM) model. VEGFR-2-IN-71 inhibits tumor growth in the HGC-27 xenograft model by inhibiting VEGFR2 and tubulin. VEGFR-2-IN-71 has low oral bioavailability in rats. VEGFR-2-IN-71 can be used in cancer research.

For research use only. We do not sell to patients.

VEGFR-2-IN-71 Chemical Structure

VEGFR-2-IN-71 Chemical Structure

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VEGFR-2-IN-71 Related Antibodies

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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Description

VEGFR-2-IN-71 is a dual VEGFR2/tubulin inhibitor. VEGFR-2-IN-71 inhibits tumor cell proliferation and induces apoptosis and cell cycle arrest. VEGFR-2-IN-71 inhibits angiogenesis in the chick chorioallantoic membrane (CAM) model. VEGFR-2-IN-71 inhibits tumor growth in the HGC-27 xenograft model by inhibiting VEGFR2 and tubulin. VEGFR-2-IN-71 has low oral bioavailability in rats. VEGFR-2-IN-71 can be used in cancer research[1].

In Vitro

VEGFR-2-IN-71 (Compound 6r) (1-128 μM, 48 hours) exhibits antitumor activity and cytotoxicity against HepG-2, HCT-116, HGC-27, MDA-MB-231, MCF-7, HA-VSMC, and GES-1 cells with IC50 values of 13.3 μM, 18.8 μM, 11.4 μM, 21.8 μM, 17.4 μM, 17.1 μM, and 16.73 μM, respectively[1].

VEGFR-2-IN-71 (0-2 μM, 24-72 hours) exhibits antiproliferative effects against HGC-27 and HepG-2 cells, achieving complete inhibition at 1.0 μM[1].

VEGFR-2-IN-71 (0-1 μM, 10 days) inhibits colony formation of HGC-27 and HepG-2 cells[1].

VEGFR-2-IN-71 (0-1 μM) inhibits VEGFR2 activity and exerts anti-tumor effects in HGC-27 cells by downregulating VEGF expression and regulating glycolysis-related enzymes HK2, PFKM, and PKM2[1].

VEGFR-2-IN-71 (0-1 μM) inhibits tubulin polymerization and disrupts microtubule dynamics in HGC-27 and HepG-2 cells[1].

VEGFR-2-IN-71 (0-1 μM) induces cell cycle arrest and apoptosis in HGC-27 cells[1].

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

VEGFR-2-IN-71 Related Antibodies

Western Blot Analysis[1]

Cell Line: HGC-27 cells
Concentration: 0 μM, 0.25 μM, 0.5 μM , 1 μM
Incubation Time: /
Result: Reduced VEGF protein expression.
Inhibited hexokinase 2 (HK2), phosphofructokinase muscle (PFKM) and pyruvate kinase M2 (PKM2) protein expression.

Apoptosis Analysis[1]

Cell Line: HGC-27 cells
Concentration: 0 μM, 0.25 μM, 0.5 μM , 1 μM
Incubation Time: /
Result: Induced cell cycle arrest at the G2/M phase and apoptosis, with the percentages of apoptotic cells at 0.25, 0.5, and 1 μM were 10.01%, 13.45%, and 16.54%, respectively.
In Vivo

VEGFR-2-IN-71 (Compound 6r) (1-10 μM, 48 hours) inhibits angiogenesis in the CAM model[1].

VEGFR-2-IN-71 (15-30 mg/kg, intraperitoneal injection, once every other day, for 16 days) exerts antitumor activity and angiogenesis inhibition in BALB/c nude mice bearing HGC-27 xenograft tumors[1].

VEGFR-2-IN-71 (20-100 mg/kg, intraperitoneal injection, once a day, for 12 days) does not damage the heart, liver, spleen, lung or kidney, and does not cause death, showing a good safety profile[1].

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

Animal Model: BALB/c nude mice (15-18 g, 5 weeks old) bearing HGC-27 xenografts model (4 × 106 cells subcutaneously implanted in the left armpit) [1]
Dosage: 15 mg/kg, 30 mg/kg
Administration: i.p., every other day, 16 days
Result: Inhibited tumor growth at 15 mg/kg, reduced the growth rates and final weights of tumors, showing an inhibitory effect on tumor growth, with the rates reaching 68.35% at 30 mg/kg.
Reduced the expression of Ki67 and MVD and inhibited angiogenesis within tumors.
Reduced the levels of VEGFA, a marker of angiogenesis, and VEGFR-2, an early marker of endothelial progenitor cells, in tumors.
Molecular Weight

532.44

Formula

C26H20F4N2O6
SMILES

COC1=C(OC)C(OC)=C(C(C=C(C2=CC=C(NC(NC3=CC=C(F)C(C(F)(F)F)=C3)=O)C=C2)O4)=O)C4=C1
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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VEGFR-2-IN-71 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:

VEGFR-2-IN-71VEGFRMicrotubule/TubulinApoptosisVascular endothelial growth factor receptornhibitorHGC-27 cellsBALB/c nude miceAnti-cancerInhibitorinhibitorinhibit

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