In vivo and in vitro effects of a HIF-1α inhibitor, RX-0047

Z. Gunnur Dikmen, Ginelle C. Gellert, Pakize Dogan, Heejeong Yoon, Bok Lee Young, Ho Ahn Chang, Jerry W. Shay

Research output: Contribution to journalArticlepeer-review

33 Scopus citations


HIF-1α plays a major role in activating gene transcription and is important for maintaining homeostasis under hypoxic conditions. Since tumors are often in a hypoxic state, HIF-1α is a potential target for the development of novel cancer therapeutics. This study was performed to determine the antitumoral efficacy of an antisense HIF-1α inhibitor, RX-0047 on different human cancer cell lines (MDA-MB 231, HME50-T, PC-3, Panc-1 and A549) in vitro. A549 lung cancer and PC-3 prostate cancer cells containing a luciferase gene reporter were used for in vivo xenograft animal models. Progressive tumor development was quantified using live animal BLI (bioluminescence imaging) in addition to ex vivo imaging and histology. All cell lines tested were sensitive to inhibition of cell growth with 10 nM and higher ranges of RX-0047, additionally RX-0047 sensitizes cells to ionizing radiation treatments. Finally, RX-0047 (30 mg/kg) inhibited the formation of human lung metastasis in xenograft mouse models and reduced tumor size in flank models.

Original languageEnglish (US)
Pages (from-to)985-994
Number of pages10
JournalJournal of Cellular Biochemistry
Issue number3
StatePublished - Jun 1 2008


  • Bioluminescence imaging
  • Cancer
  • HIF-1α
  • Hypoxia
  • RX-0047

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology


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