| Description | LTX315 acetate (Oncopore acetate) is an oncolytic peptide with potent anticancer activity, with IC50 values of 34.3 µM for MRC-5, 8.3 µM for A20, and 11 µM for AT84, respectively. |
| In vitro | LTX315 acetate 可迅速杀死癌细胞，对药物耐药性癌细胞同样有效，对红细胞无毒性，具有高血浆蛋白结合能力，并能迅速分解成无毒代谢物。 LTX315 acetate 的抗癌活性通过直接裂解质膜和使线粒体膜渗透化而导致细胞因坏死而死亡和肿瘤抗原的释放。用 LTX315 acetate 处理癌细胞会导致释放多种危险信号（DAMPs），这些信号与免疫原性细胞死亡和适应性免疫反应的激活相关[1]。 |
| In vivo | LTX315 acetate 通过肿瘤内给药导致肿瘤坏死和免疫细胞向肿瘤实质内浸润，随后在大多数动物体内实现了肿瘤的完全消退。在体外，LTX-315诱导风险相关分子模式分子（如高迁移率族蛋白B1）的释放，随后在体内上调了如白细胞介素（IL）1β、IL6和IL18等促炎细胞因子的表达。通过 LTX315 acetate 治疗而治愈的动物，对再次挑战活的B16肿瘤细胞的皮内和静脉注射显示出了保护作用[2]。 |
| Target activity | A20:8.3 µM, AT84:11 µM, MRC5:34.3 µM |
| Synonyms | LTX315醋酸盐, KKWWKKW-Dip-K-NH2 acetate, Oncopore acetate, Ruxotemitide acetate, LTX315 acetate(1345407-05-7, Free base) |
| molecular weight | 1499.84 |
| Molecular formula | C80H110N18O11 |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 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. |