Ruxotemitide (LTX 315)

For research use only.

Catalog No.S8199 Synonyms: Oncopore

Ruxotemitide (LTX 315) Chemical Structure

CAS No. 1345407-05-7

Ruxotemitide (LTX 315, Oncopore) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.

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Biological Activity

Description Ruxotemitide (LTX 315, Oncopore) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.
In vitro

LTX-315 is highly active against both murine and human melanoma cell lines in vitro. while displaying low EC50 cytotoxic activity against human red blood cells. LTX-315 has been shown to induce the release of ATP and HMGB1 in vitro, both being DAMPs involved in ICD[1].

Assay
Methods Test Index PMID
Immunofluorescence
SMAC; 

PubMed: 26378049     


Release of SMAC from mitochondria to the cytosol. U2OS cells stably transfected with SMAC-GFP fusion protein cultured for 6 or 24 h with the indicated concentrations of LTX-315, STS (standard dose: 1 μM) or CCCP (standard dose: 10 μM) and then counterstained with Hoechst 33342.

BAX ; 

PubMed: 26378049     


Aggregation of BAX-GFP in LTX-315-treated cells. U2OS cells stably expressing a TFAM-GFP fusion protein were cultured for 6 or 24 h with the indicated concentrations of LTX-315, STS (standard dose: 1 μM) or CCCP (standard dose: 10 μM) and then counterstained with Hoechst 33342.

26378049
Growth inhibition assay
Cell viability; 

PubMed: 21453492     


The dose response curve for LTX-315 is plotted as percent survival of the cells against the different peptide concentrations (μg/ml). The dotted line shows the peptide concentration killing 50% of the cells. The curves correspond to three experiments performed in triplicate ± SEM.

21453492
In vivo when syngeneic B16 melanomas are treated intralesionally, a majority of the animals (~80%) treated with LTX-315 experience a complete and long-lasting tumor regression. LTX-315 injection induces an extensive hemorrhagic necrosis of the tumor parenchyma and a massive infiltration of CD3+ T cells, indicating that the peptide induces a type of cell death that leads to an increase in the number of tumor-infiltrating lymphocytes (TILs). treatment of a single tumor with LTX-315 generates a systemic anti-tumor immune response that eradicated distant lesions and prevented reoccurrence following tumor rechallenge[1].

Protocol

Solubility (25°C)

In vitro Water 100 mg/mL (69.45 mM)
Ethanol '''-1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1439.79
Formula

C78H106N18O9

CAS No. 1345407-05-7
Storage powder
in solvent
Synonyms Oncopore
Smiles C1=CC=C(C=C1)C(C2=CC=CC=C2)C(C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CCCCN)NC(=O)C(CCCCN)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CNC8=CC=CC=C87)NC(=O)C(CCCCN)NC(=O)C(CCCCN)N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01223209 Completed Drug: LTX-315 Carcinoma Lytix Biopharma AS|Kael-GemVax Co. Ltd. August 2010 Phase 1
NCT01058616 Completed Drug: LTX-315 (Oncopore™) Cancer With Transdermal Accessible Tumour Lytix Biopharma AS|Oslo University Hospital|Karolinska University Hospital January 2010 Phase 1

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Bcl-2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID