Startseite>>LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

Katalog-Nr.GC32894

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LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2) Chemische Struktur

Cas No.: 1345407-05-7

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Sample solution is provided at 25 µL, 10mM.

Description of LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

LTX-315 is an oncolytic peptide with potent anticancer activity; inhibits MRC-5, A20 and AT84 with IC50s of 34.3, 8.3 and 11 μM, respectively.

LTX-315 is found to be equipotent against drug-resistant cancer cells, nontoxic towards red blood cells, shows high plasma protein binding and is quite rapidly degraded to non-toxic metabolites. LTX-315 induces rapid killing of cancer cells. The oncolytic activity of LTX-315 stems from both a direct lytic effect on the plasma membrane in addition to permeabilization of the mitochondrial membrane, leading to cellular death by necrosis and release of tumor antigens. Treatment of cancer cells with LTX-315 causes the release of several danger signals (DAMPs) that are associated with immunogenic cell death and stimulation of adaptive immune responses[1].

Intratumoral administration of LTX-315 has resulted in complete regression and systemic tumor specific immune responses in several preclinical models[1]. Intratumoral administration of LTX-315 resulted in tumor necrosis and the infiltration of immune cells into the tumor parenchyma followed by complete regression of the tumor in the majority of the animals. LTX-315 induced the release of danger-associated molecular pattern molecules such as the high mobility group box-1 protein in vitro and the subsequent upregulation of proinflammatory cytokines such as interleukin (IL) 1β, IL6 and IL18 in vivo. Animals cured by LTX-315 treatment are protected against a re-challenge with live B16 tumor cells both intradermally and intravenously[2].

[1]. Haug BE, et al. Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide. J Med Chem. 2016 Apr 14;59(7):2918-27. [2]. Camilio KA, et al. Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315. Cancer Immunol Immunother. 2014 Jun;63(6):601-13.

Protocol of LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

Cell experiment:

Tumor cells are incubated for 4 hours with 10 concentrations of LTX-315 in 1/4 dilution step with a top dose of 400 µM, with 1% (final concentration) Triton X-100 as positive control and FBS-free culture medium as negative control. Cell cytotoxicity is measured using the MTS assay[1].

Animal experiment:

Mice: Tumor cells are harvested, ished in RPMI-1640 and injected intradermally (i.d.) into the right side of the abdomen in C57BL/6 mice. Palpable tumors are injected i.t. with single doses of LTX-315 or LTX-328 dissolved in saline (1.0 mg peptide/50 μL saline) once a day for 3 consecutive days, and the vehicle control is saline only (0.9% NaCl in sterile water). Tumor size is measured using an electronic caliper[2].

References:

[1]. Haug BE, et al. Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide. J Med Chem. 2016 Apr 14;59(7):2918-27.
[2]. Camilio KA, et al. Complete regression and systemic protective immune responses obtained in B16 melanomas after treatment with LTX-315. Cancer Immunol Immunother. 2014 Jun;63(6):601-13.

Chemical Properties of LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

Cas No. 1345407-05-7 SDF
Canonical SMILES Lys-Lys-Trp-Trp-Lys-Lys-Trp-Dip-Lys-NH2
Formula C78H106N18O9 M.Wt 1439.79
Löslichkeit DMSO : ≥ 50 mg/mL (34.73 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.6945 mL 3.4727 mL 6.9455 mL
5 mM 0.1389 mL 0.6945 mL 1.3891 mL
10 mM 0.0695 mL 0.3473 mL 0.6945 mL
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In vivo Formulation Calculator (Clear solution) of LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)

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Average Rating: 5 ★★★★★ (Based on Reviews and 5 reference(s) in Google Scholar.)

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