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Cilengitide as an integrin targeting molecule, has shown broad application prospects in tumor therapy and related biomedical research fields. Existing research indicates that its applications mainly focus on multiple directions such as comprehensive treatment systems for malignant tumors, anti angiogenesis interventions, anti metastasis control, construction of multimodal combination therapies, and imaging and basic research.



Cilengitide COA
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| Certificate of Analysis | ||
| Compound name | Cilengitide | |
| Grade | Pharmaceutical grade | |
| CAS No. | 188968-51-6 | |
| Quantity | 40g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090088 | |
| MFG | Jan 9th 2026 | |
| EXP | Jan 8th 2029 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.54% |
| Loss on drying | ≤1.0% | 0.42% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.98% |
| Single impurity | <0.8% | 0.52% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 500ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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| Chemical Formula | C27H40N8O7 | |
| Exact Mass | 588 | |
| Molecular Weight | 589 | |
| m/z | 588 (100.0%), 589 (29.2%), 590 (4.1%), 589 (3.0%), 590 (1.4%) | |
| Elemental Analysis | C, 55.09; H, 6.85; N, 19.04; O, 19.02 | |

Application in tumor treatment system
In the field of tumor treatment, the application of cilengitide is first focused on the comprehensive treatment system of central nervous system malignant tumors, especially glioblastoma. In newly diagnosed patients, the drug is included in the standard initial treatment pathway as an important component of the combination therapy of radiotherapy and temozolomide chemotherapy, used to construct a multimodal collaborative treatment system.
In recurrent glioblastoma, its use has been further expanded to the second-line and posterior line treatment stages, as a supplementary intervention after previous treatment failures, to maintain the continued implementation of disease control strategies. In high-grade gliomas (grade III and IV), cilantrotide is integrated into a complex treatment pathway, forming a multi-level intervention structure together with radiotherapy, chemotherapy, and other treatment methods.
In the postoperative stage of brain tumor surgery, this drug is used in the postoperative adjuvant therapy system to continue the treatment pathway and maintain the continuity of overall intervention.
Meanwhile, in the process of radiotherapy, it is used in conjunction with radiotherapy methods, and in the process of chemotherapy, it is included in the combination therapy system, thus forming a continuous comprehensive intervention path in different treatment stages.
In addition to central nervous system tumors, its use in various solid tumors is also constantly expanding. In malignant melanoma, it is used as a combination therapy system for advanced and metastatic stages to support the implementation of disease control pathways. In non-small cell lung cancer, this drug is included in the comprehensive treatment plan for advanced patients and used for continued treatment interventions during the metastatic phase.
In head and neck squamous cell carcinoma, it is used as an auxiliary component in radiotherapy or chemotherapy related treatment pathways, participating in local and systemic treatment systems.In prostate cancer, breast cancer, colorectal cancer and other tumors, it is mainly used in combination treatment structures to support the implementation of the overall treatment plan. In the research fields of pancreatic cancer, hepatocellular carcinoma, ovarian cancer and renal cell carcinoma, the drug is used in exploratory treatment systems to evaluate its application potential in different tumor types.
Anti angiogenesis related uses
In the field of anti angiogenesis, its applications run through two levels: tumor treatment and basic research. In the tumor treatment system, it is used in anti angiogenesis strategies and participates in the intervention process as a component of the comprehensive treatment pathway. In the case where tumor blood vessels have already formed, this drug is used in relevant intervention research pathways to participate in vascular structure related regulatory systems. In combination therapy, it is used in conjunction with other anti angiogenic drugs to construct a multifactorial intervention structure to enhance the synergy of the overall treatment system.
In experimental and clinical studies, it has also been used as an intervention tool in the research pathway of microvascular related indicators to participate in the evaluation system of tumor angiogenesis degree. In addition, in the study of non tumor vascular abnormalities, this drug has also been used in research pathways related to angiogenesis regulation, demonstrating its application value in a wider range of vascular biology fields.
Anti metastasis and invasion control purposes
In the field of tumor metastasis and invasion research, it is widely used in related research systems. At the cellular level, it is used as an intervention tool in cell migration related research pathways to participate in cellular behavior analysis. In invasion research, this drug is used in experimental models as a research system involved in tumor invasion behavior. In transfer studies, it is included in relevant experimental and clinical research pathways to participate in the research and control strategy construction of the transfer process.
In clinical research settings, the drug is also used as an auxiliary intervention in the overall management system for the prevention of metastasis in high-risk postoperative patients. Meanwhile, in patients who have already undergone metastasis, it is used in the continuity of treatment pathway to support long-term management of the metastasis stage.
The use of multimodal combination therapy system
In modern cancer treatment, multimodal combination therapy has become an important direction of development, and cilengitide has a wide range of uses in such systems. In the radiotherapy combination system, it is used to jointly construct a collaborative intervention pathway with radiotherapy methods. In the chemotherapy combination system, the drug is incorporated into a multi drug combination structure and participates in the systemic treatment pathway.
In targeted therapy systems, it is used in multi-target combination therapy strategies as part of a comprehensive intervention structure to participate in the treatment process.
In addition, it has also been used in immunotherapy research to explore pathways for combination therapy and to support the construction of multimodal treatment systems. In the design of complex treatment pathways, this drug is used for multi-stage and multi strategy combination applications, and plays an important role in connecting different treatment stages in a sequential treatment system.
Imaging and diagnostic related applications
In the field of imaging research, it is used as a marker molecule in molecular imaging research systems to participate in integrin targeted imaging pathways. In tumor research, it is used in angiogenesis related imaging evaluation systems to analyze tumor activity and vascular changes. In clinical studies, the drug has also been used in the dynamic monitoring pathway of treatment response to evaluate the trend of disease changes during the treatment process.
Meanwhile, in prognostic assessment research, it is used as a research tool in relevant analysis systems to evaluate the relationship between disease progression and prognosis. In addition, it is also used in patient screening related research pathways to support the development of precision treatment strategies.

Basic research and translational medicine applications
In the field of basic research, as a classic integrin related research tool, it is widely used in the research systems of cell biology and tumor biology. It is used for integrin function research, cell adhesion research, and cell migration experimental model construction, and is used in tumor microenvironment research to analyze the interrelationships between tumors, blood vessels, and matrix. In the study of signaling pathways, this drug is used in the research system of integrin related pathways.
In the field of drug development, it is used as a tool molecule in new drug screening systems and in animal models to validate relevant therapeutic pathways. In translational medicine research, this drug is used as a bridge between basic research and clinical applications to support the translation of experimental research into clinical practice.
Use in other disease research
In the research of diseases other than tumors, its applications are constantly expanding. In the study of ophthalmic diseases, it is used in research pathways related to abnormal angiogenesis, including macular degeneration and retinopathy. In inflammation related diseases, this drug is used in research systems related to vascular changes. In the study of autoimmune diseases, it is used as a pathway for investigating immune related cell behavior.
In anti fibrotic research, Cilengitide is used in tissue fibrosis related research systems. In the research of cardiovascular disease, it is used in the research path of vascular remodeling and abnormal changes, and is applied in the model of atherosclerosis. In addition, in the fields of tissue engineering and regenerative medicine, this drug is used to regulate the interaction between cells and matrix, and is applied in research pathways related to neovascularization.
References
1. Stupp R, et al. Clinical trials of cilengitide in glioblastoma. Journal of Clinical Oncology
2. Nabors LB, et al. Phase I/II studies of cilengitide
3. Desgrosellier JS, Cheresh DA. Integrins in cancer. Nature Reviews Cancer
4. ClinicalTrials.gov (keyword: Cilengitide)
5. Nature Reviews Drug Discovery
6. The Lancet Oncology (related research)
7. Goodman & Gilman's The Pharmacological Basis of Therapeutics
FAQ
What is cilengitide?
A cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.
What is the half life of cilengitide?
Additionally, cilengitide has a short plasma half-life of 3-5 hours and has a clearance of 34-66 mL/min/m2, with no evidence of metabolism, drug accumulation, or enterohepatic circulation.
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