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PX 478

Known as: L-Phenylalanine, 4-[Bis(2-chloroethyl)oxidoamino]-, Dihydrochloride; L-Phenylalanine, 4-[Bis(2-chloroethyl)oxidoamino]-, Hydrochloride (1:2), PX-478, (S)-4-(2-Amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline Oxide Dihydrochloride 
An orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha… 
National Institutes of Health

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NCIt Antineoplastic Agent Terminology

Papers overview

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2018
2018
Notch signaling pathway regulates cell cycle in proliferating hepatocytes involved in liver regeneration
It has been well documented that Notch signaling is involved in liver regeneration. However, the exact molecular mechanism… 
Highly Cited
2017
Highly Cited
2017
Canonical hedgehog signalling regulates hepatic stellate cell‐mediated angiogenesis in liver fibrosis
Hepatic stellate cells (HSCs) are liver‐specific pericytes regulating angiogenesis during liver fibrosis. We aimed to elucidate… 
2014
2014
Binge alcohol promotes hypoxic liver injury through a CYP2E1-HIF-1α-dependent apoptosis pathway in mice and humans.
Highly Cited
2012
Highly Cited
2012
Selective Inhibition of Hypoxia-Inducible Factor 1α Ameliorates Adipose Tissue Dysfunction
ABSTRACT Hypoxia-inducible factor 1α (HIF1α) induction in adipocytes is a critical component of the “fibrotic response,” directly… 
Highly Cited
2010
Highly Cited
2010
Radiosensitization and Stromal Imaging Response Correlates for the HIF-1 Inhibitor PX-478 Given with or without Chemotherapy in Pancreatic Cancer
Growing tumors are hypoxic and respond to microenvironmental stress through increased expression of the hypoxia inducible factor… 
2010
2010
Results from a phase I, dose-escalation study of PX-478, an orally available inhibitor of HIF-1{alpha}.
3076 Background: Hypoxia inducible factor-1 (HIF-1) transcription factor is an important regulator of cellular response to… 
Highly Cited
2009
Highly Cited
2009
The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects
Hypoxia inducible factor-1 (HIF-1) promotes tumor cell adaptation to microenvironmental stress. HIF-1 is up-regulated in… 
Highly Cited
2008
Highly Cited
2008
Regulation of the Warburg effect in early-passage breast cancer cells.
Malignancy in cancer is associated with aerobic glycolysis (Warburg effect) evidenced by increased trapping of [(18)F… 
Highly Cited
2005
Highly Cited
2005
Dynamic contrast-enhanced and diffusion MRI show rapid and dramatic changes in tumor microenvironment in response to inhibition of HIF-1alpha using PX-478.
PX-478 is a new agent known to inhibit the hypoxia-responsive transcription factor, HIF-1alpha, in experimental tumors. The… 
Highly Cited
2005
Highly Cited
2005
Metabolite changes in HT‐29 xenograft tumors following HIF‐1α inhibition with PX‐478 as studied by MR spectroscopy in vivo and ex vivo
The hypoxia‐inducible transcription factor (HIF‐1α) plays a central role in tumor development. PX‐478 is an experimental anti… 
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