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Merck
CN

SML3962

LTX-315 trifluoroacetate

≥95% (HPLC)

Synonym(s):

KKWWKKW(Dip)K-NH2 trifluoroacetate, LTX 315 trifluoroacetate, LTX-315 trifluoroacetate, Lys-Lys-Trp-Trp-Lys-Lys-Trp-Dip-Lys-NH2 (Dip = 3,3-diphenylalanine) trifluoroacetate, Ruxotemitide trifluoroacetate

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About This Item

Empirical Formula (Hill Notation):
C78H106N18O9
Molecular Weight:
1439.79
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

assay

≥95% (HPLC)

form

(Powder or Lyophilized powder or film)

storage condition

desiccated

color

white to off-white

storage temp.

-10 to -25°C

Quality Level

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.

Disclaimer

Hygroscopic

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

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The oncolytic peptide LTX-315 overcomes resistance of cancers to immunotherapy with CTLA4 checkpoint blockade
Cell Death and Differentiation, 23(6), 1004-1015 (2016)
The oncolytic peptide LTX-315 kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization
Oncotarget, 6(29), 26599-26614 (2015)
Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315
Cancer Immunology, Immunotherapy, 63(6), 601-613 (2014)
LTX-315 (Oncopore?): A short synthetic anticancer peptide and novel immunotherapeutic agent
Oncoimmunology (2014)
The oncolytic peptide LTX-315 triggers immunogenic cell death
Cell Death & Disease, 7(3) (2016)

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