LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)是一种阳离子两亲性肽，它能快速使线粒体膜发生通透性改变，从而引发部分由BAX/BAK1控制、且不依赖于半胱天冬酶的细胞坏死。
Cas No.:1345407-05-7
Sample solution is provided at 25 µL, 10mM.
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LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2) is a cationic amphilytic peptide that preferentially permeabilizes mitochondrial membranes, thereby causing partially BAX/BAK1-regulated, caspase-independent necrosis[1].
In vitro，The IC50 value for LTX-315 was 30μM after only 5 minutes of exposure and lowered to 17μM after 60 minutes on A375 melanoma cells, and treated cells displayed a rapid change from a normal epithelial morphology to a total collapse of the cells with an extrusion of cytoplasmic content [2]. LTX-315 (0-200μg/ml) dissipated the inner mitochondrial transmembrane potential (Δψm) of U2OS cells, but could not completely dissipate U2OS cells those stably expressing a TFAM-GFP fusion [3].
In vivo, LTX-315 strongly inhibited tumor growth in B16-bearing mice, but not in B16-bearing MyD88-/- mice [4]. LTX-315 (1mg peptide/injection; twice; i.t.) combined with liposomal doxorubicin (8mg/kg body weight; twice; i.t.) produced a significant additive antitumor effect, with 50% of animals achieving complete remission; it also enhanced tumor necrosis, increased CD4+/CD8+ cell infiltration, and prolonged survival in 4T1 mammary carcinomas mouse model [5].
References:
[1]. Zhou, Heng, et al. "The oncolytic peptide LTX-315 triggers immunogenic cell death." Cell death & disease 7.3 (2016): e2134-e2134.
[2]. Eike, Liv-Marie, et al. "The oncolytic peptide LTX-315 induces cell death and DAMP release by mitochondria distortion in human melanoma cells." Oncotarget 6.33 (2015): 34910.
[3]. Zhou, Heng, et al. "The oncolytic peptide LTX-315 kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization." Oncotarget 6.29 (2015): 26599.
[4]. Li, Xiao-Qing, et al. "LTX-315 triggers anticancer immunity by inducing MyD88-dependent maturation of dendritic cells." Frontiers in Immunology 15 (2024): 1332922.
[5]. Camilio, Ketil A., et al. "Combining the oncolytic peptide LTX-315 with doxorubicin demonstrates therapeutic potential in a triple-negative breast cancer model." Breast Cancer Research 21.1 (2019): 9.
LTX-315 (K-K-W-W-K-K-W-Dip-K-NH2)是一种阳离子两亲性肽，它能快速使线粒体膜发生通透性改变，从而引发部分由BAX/BAK1控制、且不依赖于半胱天冬酶的细胞坏死[1]。
在体外实验中，在A375黑色素瘤细胞中，LTX-315的IC₅₀值在处理5分钟后为30μM，处理60分钟后降至17μM。并且处理后的细胞会迅速从正常的上皮形态转变为细胞完全崩解，并伴有细胞质内容物的外排[2]。LTX-315（0–200μg/mL）消除了U2OS细胞的线粒体内膜跨膜电位（Δψm），但对于稳定表达TFAM-GFP融合蛋白的U2OS细胞，无法完全消除其Δψm[3]。
在体内实验中，LTX-315可显著抑制B16荷瘤小鼠的肿瘤生长，但在B16荷瘤的MyD88-/-小鼠中则无明显作用[4]。在4T1乳腺癌小鼠模型中，LTX-315（1mg/次；瘤内注射；共2次）联合脂质体多柔比星（8mg/kg体重；共2次；瘤内注射）产生了显著的协同抗肿瘤作用，50%的动物达到完全缓解；同时增强了肿瘤坏死，增加了CD4+/CD8+细胞浸润，并延长了动物生存期[5]。
| Cell experiment [1]: | |
Cell lines | U2OS cells |
Preparation Method | 5×103 U2OS cells stably expressing PARKIN-RFP; SMAC-GFP; LC3-RFP; TFAM-GFP; BAX-GFP or Mito-RFP were seeded into black 96-well clear imaging plate and allowed to adapt for 24h. Thereafter the cells were treated with LTX-315 and respective controls and incubated for additional 6 or 24h. |
Reaction Conditions | 0-200μg/ml; 6 or 24h. |
Applications | LTX-315 dissipated the inner mitochondrial transmembrane potential (Δψm) of U2OS cells, but could not completely dissipate U2OS cells those stably expressing a TFAM-GFP fusion. |
| Animal experiment [2]: | |
Animal models | C57BL/6J or congenic MyD88-/- mice |
Preparation Method | C57BL/6J or congenic MyD88-/- mice were subcutaneously inoculated into the right flank with 1.5×105 mouse melanoma B16F10 cells to allow the formation of melanoma. B16-bearing mice with a size of 0.2-0.3cm in diameter were intratumorally injected with 3 doses (1mg/50µl PBS/injection) of LTX-315 on consecutive days, and the tumor growth was monitored. Tumor-bearing-mice were euthanized when the tumor reached 2cm in diameter or if the mouse exhibited 20% weight loss or appeared obviously stressed. |
Dosage form | 1mg/50µl/mouse; 3d; i.t. |
Applications | LTX-315 strongly inhibited tumor growth in WT mice, while the effect was partially lost in MyD88-/- mice. |
References: | |
| Cas No. | 1345407-05-7 | SDF | |
| Canonical SMILES | Lys-Lys-Trp-Trp-Lys-Lys-Trp-Dip-Lys-NH2 | ||
| 分子式 | C78H106N18O9 | 分子量 | 1439.79 |
| 溶解度 | DMSO : ≥ 50 mg/mL (34.73 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 694.5 μL | 3.4727 mL | 6.9455 mL |
| 5 mM | 138.9 μL | 694.5 μL | 1.3891 mL |
| 10 mM | 69.5 μL | 347.3 μL | 694.5 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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