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Updated: Dec 2, 2025

Development and Maintenance of a Preclinical Patient Derived Tumor Xenograft Model for the Investigation of Novel Anti-Cancer Therapies
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Therapeutic Potential of Apatinib Against Colorectal Cancer by Inhibiting VEGFR2-Mediated Angiogenesis and β-Catenin

Xiaomin Cai1, Bin Wei1,2, Lele Li1

  • 1Department of Oncology, The First Affiliated Hospital of Nanjing Medical University, Nanjing, People's Republic of China.

Oncotargets and Therapy
|November 6, 2020
PubMed
Abstract

Insights

Apatinib, a VEGFR2 inhibitor, effectively suppresses colorectal cancer (CRC) growth by blocking the VEGFR2-β-catenin pathway. This targeted therapy shows promise for treating CRC by inhibiting cell proliferation, migration, and angiogenesis.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Apatinib is a targeted therapy inhibiting vascular endothelial growth factor receptor 2 (VEGFR2).
  • Colorectal cancer (CRC) remains a significant global health challenge requiring novel therapeutic strategies.

Purpose of the Study:

  • To investigate the therapeutic efficacy of apatinib against colorectal cancer (CRC).
  • To elucidate the molecular mechanisms underlying apatinib's anti-cancer effects in CRC.

Main Methods:

  • In vivo and in vitro assays were performed to assess apatinib's impact on CRC.
  • RNA-sequencing (transcriptome) analysis was utilized to explore the mechanism of action in apatinib-treated HCT116 cells.

Main Results:

  • Apatinib demonstrated significant antiproliferative and proapoptotic effects, induced G0/G1 cell cycle arrest, and inhibited CRC cell migration and invasion.
  • Apatinib treatment led to decreased levels of p-Src, p-Akt, and p-GSK3β via VEGFR2 inhibition, increasing β-catenin ubiquitination and reducing its nuclear translocation.
  • In vivo studies showed apatinib suppressed CT26 tumor growth in mouse xenograft models by inhibiting β-catenin signaling and angiogenesis.

Conclusions:

  • Apatinib effectively inhibits the VEGFR2-β-catenin pathway, suppressing the malignant phenotype in CRC.
  • Apatinib demonstrates significant potential as a therapeutic strategy for colorectal cancer treatment.
Keywords:
VEGFR2angiogenesisapatinibcolorectal cancerβ-catenin

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