APTO-253 (LOR253 HCl) - CAS 1422731-37-0
Catalog number: 1422731-37-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
APTO-253, also known as LOR-253, LT-253,  is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-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.
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Appearance:
Solid powder
Synonyms:
APTO-253; APTO 253; APTO253; LOR253; LOR-253; LOR 253; LT-253.
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Current Developer:
Aptose Biosciences / Lorus Therapeutics Inc.
1.Phase 1 study of APTO-253 HCl, an inducer of KLF4, in patients with advanced or metastatic solid tumors.
Cercek A1, Wheler J2, Murray PE3, Zhou S3, Saltz L4. Invest New Drugs. 2015 Oct;33(5):1086-92. doi: 10.1007/s10637-015-0273-z. Epub 2015 Aug 14.
INTRODUCTION: This phase I, multicenter, open-label, single-arm, dose-escalation study evaluated the safety, pharmacokinetics and antitumor activity of APTO-253, an inducer of the transcription factor KLF4, in adults with advanced solid tumors.
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CAS 1422731-37-0 APTO-253 (LOR253 HCl)

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