Certepetide
(Synonyms: CEND-1; iRGD) 目录号 : GC68856Certepetide(CEND-1)是一种新型的靶向肿瘤的内化精氨酸甘氨酸双功能环肽(a.k.a. iRGD)，正在开发用于治疗实体瘤。
Cas No.:2580154-02-3
Sample solution is provided at 25 µL, 10mM.
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Certepetide (CEND-1) is a novel tumor-targeting internalized arginine-glycine bifunctional cyclic peptide (a.k.a. iRGD), which is being developed for the treatment of solid tumors[1]. Certepetide aims to overcome the existing challenges in the treatment of solid tumors by delivering combined anti-cancer drugs into tumors, selectively consuming immunosuppressive T cells, enhancing the killing ability of toxic T cells in the tumor microenvironment, and inhibiting the metastatic cascade reaction[2,3].
In vitro, when GFP-PC-3 and LM-PmC tumor cells were treated with Certepetide (10μM) for 24 hours, the random migration ability of LM-PmC and GFP-PC-3 cells in vitro was significantly inhibited, which was helpful in preventing the initial metastasis of tumor cells[2].
In vivo, Certepetide (4μmol/kg) was administered via tail vein injection in the mouse subcutaneous tumor model of liver cancer established by subcutaneous injection of HepG2 or Huh-7 cells (liver cancer cells). Certepetide can increase the concentration of sorafenib in subcutaneous tumor tissues without increasing systemic toxic effects. And enhance the killing ability of toxic T cells[4,5].
References:
[1]Winning A, Sietsema WK, Buck KK, Linsmeier A, Wiczling P. Population Pharmacokinetic Modeling of Certepetide in Human Subjects With Metastatic Pancreatic Ductal Adenocarcinoma. Clin Pharmacol Drug Dev. 2025 Mar;14(3):240-251.
[2] Sugahara KN, Teesalu T, Karmali PP, Kotamraju VR, Agemy L, Girard OM, Hanahan D, Mattrey RF, Ruoslahti E. Tissue-penetrating delivery of compounds and nanoparticles into tumors. Cancer Cell. 2009 Dec 8;16(6):510-20.
[3] Teesalu T, Sugahara KN, Kotamraju VR, Ruoslahti E. C-end rule peptides mediate neuropilin-1-dependent cell, vascular, and tissue penetration. Proc Natl Acad Sci U S A. 2009 Sep 22;106(38):16157-62.
[4] Schmithals C, Köberle V, Korkusuz H, Pleli T, Kakoschky B, Augusto EA, Ibrahim AA, Arencibia JM, Vafaizadeh V, Groner B, Korf HW, Kronenberger B, Zeuzem S, Vogl TJ, Waidmann O, Piiper A. Improving Drug Penetrability with iRGD Leverages the Therapeutic Response to Sorafenib and Doxorubicin in Hepatocellular Carcinoma. Cancer Res. 2015 Aug 1;75(15):3147-54.
[5] McEwen A., Henson C. Quantitative whole-body autoradiography: Past, present and future. Bioanalysis. 2015;7:557–568.
Certepetide(CEND-1)是一种新型的靶向肿瘤的内化精氨酸甘氨酸双功能环肽(a.k.a. iRGD)，正在开发用于治疗实体瘤[1]。Certepetide 旨在通过将联合给药的抗癌药物输送到肿瘤中，同时选择性地消耗免疫抑制性T细胞，增强肿瘤微环境中的毒性T细胞杀伤能力，并抑制转移级联反应，从而克服治疗实体瘤的现有挑战[2,3]。
在体外，Certepetide（10μM）处理GFP-PC-3和LM-PmC肿瘤细胞24小时，显著抑制了LM-PmC和GFP-PC-3细胞的体外随机迁移能力，有助于预防肿瘤细胞初始转移[2]。
在体内，Certepetide（4μmol/kg）尾静脉注射给药于通过皮下注射HepG2或Huh-7细胞（肝癌细胞）建立的小鼠肝癌皮下瘤模型，Certepetide能提高索拉菲尼在皮下肿瘤组织的浓度，且不会增加全身毒性作用，并增强毒性T细胞的杀伤能力[4,5]。
| Cell experiment [1]: | |
Cell lines | GFP-PC-3 cells; LM-PmC cells |
Preparation Method | Cell migration was analyzed using 24-well Transwell chambers containing polycarbonate membranes with 8-μm pores. Both sides of the membranes were coated with 50μg/ml of collagen type-I to facilitate initial cell attachment to the membranes. GFP-PC-3 (4 × 104 cells) or LM-PmC (2 × 105 cells) cells in DMEM containing 0.1% BSA were added to the upper compartment. The lower compartment was filled with 600μl of DMEM containing 0.1% BSA. Certepetide at a final concentration of 10μM or PBS were added to both the upper and lower compartments. The total number of cells that migrated to the lower side of the membranes was determined by counting cell numbers under low magnification. |
Reaction Conditions | 10μM; 24h |
Applications | Certepetide can inhibit the in vitro random migration ability of LM-PmC and GFP-PC-3 tumor cells, which is helpful in preventing the initial metastasis of tumor cells. |
| Animal experiment [2]: | |
Animal models | Nude mice |
Preparation Method | A total of 5 × 106 HepG2 or Huh-7 cells (resuspended in 100μL of PBS) was injected subcutaneously into nude mice. Three to 4 weeks later, the mice were assigned to the treatment groups. Doxorubicin was dissolved in PBS and sorafenib in a vehicle containing 12.5% Cremophor and 12.5% ethanol. Nude mice bearing HepG2 or Huh-7 xenografts received Certepetide (4μmol/kg by tail vein injection), or PBS 15 minutes each time before treatment with doxorubicin (3mg/kg, 3 times per week intraperitoneally) or sorafenib (every second day orally). Body weight and tumor size were determined every 2 to 3 days with a caliper. At the end of the experiment, the mice were sacrificed by cervical dislocation. Tumors were excised and weighed. |
Dosage form | 4μmol/kg; 28 days; i.v. |
Applications | Certepetide can increase the concentration of sorafenib in subcutaneous tumor tissues without increasing systemic toxic effects and enhancing the killing ability of toxic T cells |
References: | |
| Cas No. | 2580154-02-3 | SDF | Download SDF |
| 别名 | CEND-1; iRGD | ||
| 分子式 | C37H60N14O14S2 | 分子量 | 989.09 |
| 溶解度 | 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 | 1.011 mL | 5.0552 mL | 10.1103 mL |
| 5 mM | 0.2022 mL | 1.011 mL | 2.0221 mL |
| 10 mM | 0.1011 mL | 0.5055 mL | 1.011 mL |
| 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: >99.00%
- COA (Certificate Of Analysis)
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