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Biochem/physiol Actions
Mitochondrial membrane-permeabilizing cationic oncolytic peptide with cancer-selective cytotoxicity in cultures and in vivo.
LTX-315 (Ruxotemitide) is a 9-mer cationic oncolytic peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis. LTX-315 exhibits cancer-selective cytotoxicity (IC50 = 1.2-7.2 μM among 47 cancer lines; normal MRC-5/HUVEC-C/RBC IC50 = 9.2/16.3/695 μM) with low inhibitory potency toward CYP450 enzymes (IC50 from 7.9 to >100 μM). Intratumoral administration results in B16 melanoma tumor necrosis and the infiltration of immune cells into the tumor parenchyma followed by complete tumor regression in mice in vivo (1 mg/50 μL i.t.). Animals cured by LTX-315 treatment are protected against B16 tumor cells re-challenge.
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Hygroscopic
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | (Powder or Lyophilized powder or film) |
| storage condition | desiccated |
| color | white to off-white |
| storage temp. | -10 to -25°C |
| SMILES string | [nH]1c2c(c(c1)C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)CCCCN)CCCCN)Cc7c8c([nH]c7)cccc8)Cc5c6c([nH]c5)cccc6)CCCCN)CCCCN)C(=O)N[C@@H](C(c4ccccc4)c3ccccc3)C(=O)N[C@@H](CCCCN)C(=O)N)cccc2 |
| InChI key | GGAKLYWEFZCVIT-TVEKFXMRSA-N |
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