iRGD peptide (c(CRGDKGPDC))
(Synonyms: c(CRGDKGPDC)) 目录号 : GC32787
iRGD peptide (c(CRGDKGPDC))是一种由9个氨基酸组成的环状肽，能够特异性结合av整合素，然后被酶解产生CRGDK/R与神经纤毛蛋白-1（NRP-1）相互作用，从而触发药物的组织渗透，具有肿瘤靶向和肿瘤穿透特性。
Cas No.:1392278-76-0
Sample solution is provided at 25 µL, 10mM.
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iRGD peptide (c(CRGDKGPDC)) is a cyclic peptide composed of 9 amino acids that can specifically bind to av integrin and then be enzymatically hydrolyzed to produce CRGDK/R, which interacts with neuropilin-1 (NRP-1), thereby triggering drug tissue penetration and having tumor targeting and tumor penetration properties[1]. iRGD peptide is a promising cancer imaging peptide and a potential therapeutic agent for a variety of cancers. iRGD peptide can effectively and deeply deliver imaging agents and anticancer drugs into tumors[2]. iRGD peptide does not affect the survival of tumor cells, but can inhibit spontaneous tumor metastasis[3].
In vitro, iRGD peptide (64μM) treatment of A549 cells for 1h significantly enhanced the membrane permeability induced by low concentrations of HPRP-A1 (4μM, 8μM) and improved the anticancer activity of HPRP-A1[4].
In vivo, iRGD peptide (4mmol/kg) was intravenously injected into mice bearing HCG27 and NCI-N87 cell xenografts for 4 weeks, significantly enhancing the chemotherapeutic effect of 5-FU and inhibiting the growth rate of tumors in both tumor-bearing mice[5]. iRGD peptide (4mg/kg) was intravenously injected into mice bearing A549 cell xenografts for 30 days, significantly enhancing the chemotherapeutic effect of gemcitabine, inhibiting tumor cell proliferation and inducing cell apoptosis[6].
References:
[1] Thirumalai A, Girigoswami K, Pallavi P, et al. Cancer therapy with iRGD as a tumor-penetrating peptide[J]. Bulletin du Cancer, 2023, 110(12): 1288-1300.
[2] Zuo H. iRGD: a promising peptide for cancer imaging and a potential therapeutic agent for various cancers[J]. Journal of oncology, 2019, 2019(1): 9367845.
[3] Yin H, Yang J, Zhang Q, et al. iRGD as a tumor‑penetrating peptide for cancer therapy[J]. Molecular medicine reports, 2017, 15(5): 2925-2930.
[4] Hu C, Chen X, Huang Y, et al. Co-administration of iRGD with peptide HPRP-A1 to improve anticancer activity and membrane penetrability[J]. Scientific reports, 2018, 8(1): 2274.
[5] Zhang L I, Xing Y, Gao Q I, et al. Combination of NRP1-mediated iRGD with 5-fluorouracil suppresses proliferation, migration and invasion of gastric cancer cells[J]. Biomedicine & Pharmacotherapy, 2017, 93: 1136-1143.
[6] Zhang Q, Zhang Y, Li K, et al. A novel strategy to improve the therapeutic efficacy of gemcitabine for non-small cell lung cancer by the tumor-penetrating peptide iRGD[J]. PLoS One, 2015, 10(6): e0129865.
iRGD peptide (c(CRGDKGPDC))是一种由9个氨基酸组成的环状肽，能够特异性结合av整合素，然后被酶解产生CRGDK/R与神经纤毛蛋白-1（NRP-1）相互作用，从而触发药物的组织渗透，具有肿瘤靶向和肿瘤穿透特性[1]。iRGD peptide是一种有前景的癌症成像肽和多种癌症的潜在治疗剂，可以将成像剂和抗癌药物有效而深入地递送到肿瘤内[2]。iRGD peptide不影响肿瘤细胞的存活，但能够抑制自发性肿瘤转移[3]。
在体外，iRGD peptide（64μM）处理A549细胞1h，显著增强了低浓度下HPRP-A1（4μM、8μM）诱导的膜通透性，提高了HPRP-A1的抗癌活性[4]。
在体内，iRGD peptide（4mmol/kg）通过静脉注射治疗HCG27和NCI-N87细胞异种移植小鼠4周，显著增强了5-FU的化疗效果，抑制了两种荷瘤小鼠体内肿瘤的生长速度[5]。iRGD peptide（4mg/kg）通过静脉注射治疗A549细胞异种移植小鼠30天，显著增强了吉西他滨（Gemcitabine）的化疗效果，抑制了肿瘤细胞增殖、诱导了细胞凋亡[6]。
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | Membrane disruption in A549 cells by peptides. A549 cells were cultured with 4μM, 8μM or 16μM HPRP-A1 with or without 64μM iRGD peptide for 1h. Next, 5μL PI was added and cells were incubated for 30min. The fluorescence of PI was measured by flow cytometry. |
Reaction Conditions | 64μM; 1h |
Applications | iRGD peptide significantly potentiates HPRP-A1-induced membrane permeabilization at low-to-moderate HPRP-A1 concentrations but has no additive effect at saturating (16μM) doses. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | 12 male BALB/c nude mice (4 weeks old) were divided into 4 groups, 3 mice in each group. Two groups were injected subcutaneously with 3×106 HCG27 cells in the flank, and the other two groups were injected subcutaneously with NCI-N87 cells. The experimental group was injected intravenously with 5-FU (25mg/kg) mixed with iRGD peptide (4mmol/kg) every 3 days for 4 weeks; the control group was injected with 5-FU (25mg/kg) mixed with PBS. Tumor volume was measured with a vernier caliper every week. |
Dosage form | 4mmol/kg; every 3 days for 4 weeks; i.v. |
Applications | In the 5-FU+iRGD peptide treatment group, the growth rates of both HCG27- and NCI-N87-induced subcutaneous tumors were significantly slower, and their weights were lighter compared to controls. |
References: | |
| Cas No. | 1392278-76-0 | SDF | |
| 别名 | c(CRGDKGPDC) | ||
| Canonical SMILES | Cyclo(Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys) | ||
| 分子式 | C35H57N13O14S2 | 分子量 | 948.04 |
| 溶解度 | Water : ≥ 50 mg/mL (52.74 mM) | 储存条件 | -20°C, protect from light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.0548 mL | 5.274 mL | 10.5481 mL |
| 5 mM | 0.211 mL | 1.0548 mL | 2.1096 mL |
| 10 mM | 0.1055 mL | 0.5274 mL | 1.0548 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)
- SDS (Safety Data Sheet)
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