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apto-253

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Overview

NCI Definition [1]:
The hydrochloride salt of a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor APTO-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.

Clinical Trials

View Clinical Trials for apto-253

Apto-253 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating apto-253, 1 is phase 1 (1 open).

Complex karyotype, Loss of Y, and Monosomy 7 are the most frequent biomarker inclusion criteria for apto-253 clinical trials.

Acute myeloid leukemia and myelodysplastic syndromes are the most common diseases being investigated in apto-253 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Apto-253
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating apto-253 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
mtf-1 inhibitor lor-253 hcl, apto-253 hcl, lt-253 hcl, 2-(6-fluoro-2-methyl-1h-indol-3-yl)-1h-imidazo[4,5-f][1,10]phenanthroline hydrochloride, mtf-1 inhibitor apto-253 hcl, lor-253 hcl, 1422731-37-0, mtf-1 inhibitor lor-253 hcl, 2-(6-fluoro-2-methyl-1h-indol-3-yl)-1h-imidazo[4,5-f][1,10]phenanthroline hydrochloride, mtf-1 inhibitor apto-253 hcl
Drug Target(s) [2]:
MTF1
NCIT ID [1]:
C95724

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.