Cilengitide (Synonyms: EMD 121974) |
Katalog-Nr.GC13559
One-Click Copy Product Info
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Cilengitide (EMD 121974) ist ein potenter und selektiver Inhibitor der Integrine αΝβ3 und αΝβ5. Cilengitide hemmt die Bindung von isoliertem αΝβ3 und αΝβ5 an Vitronectin mit einem IC50-Wert von 4 bzw. 79 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 188968-51-6
Sample solution is provided at 25 µL, 10mM.
Cilengitide, a cyclized pentapeptide, is a potent integrins antagonist with IC50 values of 0.61nM, 8.4nM and 14.9nM for ανβ3, ανβ5, and α5β1, respectively[1]. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to vitronectin with an IC50 value of 4 and 79nM, respectively[2]. Cilengitide targets integrin dimers ITGAV:ITGB3 and ITGAV:ITGB5, and induces death in breast cancer cells with low integrin abundance[3]. Cilengitide has been widely used in various cancer cell models to block integrin-mediated cell adhesion and migration[4].
In vitro, Cilengitide treatment for 24 hours significantly inhibited the viability of A375 cells, with an IC50 value of 5µg/ml[5]. Treatment with 50μg/ml Cilengitide for 72 hours significantly inhibited the adhesion of HMEC-1 endothelial cells on the culture dish and induced cell apoptosis[6]. Treatment with 100μg/ml Cilengitide for 3 days significantly inhibited the proliferation, migration and invasion of MDA-MB-231 cells[7].
In vivo, Cilengitide treatment via daily intraperitoneal injection at a dose of 75mg/kg/day for 10 days, combined with two brain X-ray irradiations (5Gy; on the third and sixth days after tumor establishment), significantly inhibited the growth of brain tumors in mice and reduced tongue-like brain invasion[8]. Forty-eight hours after a single intraperitoneal injection of 4mg/kg of Cilengitide into a rat model of glioma xenografts, significant autophagy was induced in the xenograft tumors[9].
References:
[1] Kapp T G, Rechenmacher F, Neubauer S, et al. A comprehensive evaluation of the activity and selectivity profile of ligands for RGD-binding integrins[J]. Scientific reports, 2017, 7(1): 39805.
[2] Hariharan S, Gustafson D, Holden S, et al. Assessment of the biological and pharmacological effects of the ανβ3 and ανβ5 integrin receptor antagonist, cilengitide (EMD 121974), in patients with advanced solid tumors[J]. Annals of oncology, 2007, 18(8): 1400-1407.
[3] Girnius N, Henstridge A Z, Marks B, et al. Cilengitide sensitivity is predicted by overall integrin expression in breast cancer[J]. Breast Cancer Research, 2024, 26(1): 187.
[4] Reardon D A, Nabors L B, Stupp R, et al. Cilengitide: an integrin-targeting arginine–glycine–aspartic acid peptide with promising activity for glioblastoma multiforme[J]. Expert opinion on investigational drugs, 2008, 17(8): 1225-1235.
[5] Pan X, Yi M, Liu C, et al. Cilengitide, an αvβ3-integrin inhibitor, enhances the efficacy of anti-programmed cell death-1 therapy in a murine melanoma model[J]. Bioengineered, 2022, 13(2): 4557-4572.
[6] Oliveira-Ferrer L, Hauschild J, Fiedler W, et al. Cilengitide induces cellular detachment and apoptosis in endothelial and glioma cells mediated by inhibition of FAK/src/AKT pathway[J]. Journal of Experimental & Clinical Cancer Research, 2008, 27(1): 86.
[7] Bretschi M, Merz M, Komljenovic D, et al. Cilengitide inhibits metastatic bone colonization in a nude rat model[J]. Oncology reports, 2011, 26(4): 843-851.
[8] Wilisch-Neumann A, Kliese N, Pachow D, et al. The integrin inhibitor cilengitide affects meningioma cell motility and invasion[J]. Clinical Cancer Research, 2013, 19(19): 5402-5412.
[9] Lomonaco S L, Finniss S, Xiang C, et al. Cilengitide induces autophagy-mediated cell death in glioma cells[J]. Neuro-oncology, 2011, 13(8): 857-865.
| Cell experiment [1]: | |
Cell lines | A375 cells |
Preparation Method | A375 cells were cultured in Dulbecco Modified Eagle Medium (DMEM) containing 10% fetal bovine serum (FBS) at 37°C and 5% CO2 in a CO2 incubator. The cells (6×103 per well) were seeded in a 96-well plate and cultured overnight. Subsequently, the cells were treated with Cilengitide at concentrations of 0, 1, 10, 100, and 1000µg/ml. At 24 hours, 48 hours, and 72 hours after treatment, 10µl of CCK-8 cell counting reagent was added to each well. After incubation at 37°C and 5% CO2 for 2 hours, the absorbance value was measured at a wavelength of 450nm. |
Reaction Conditions | 0, 1, 10, 100, and 1000µg/ml; 24, 48, and 72h |
Applications | Cilengitide treatment reduced cell viability of A375 cells in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Nude rats |
Preparation Method | Cells expressing light chain (LC) 3-green fluorescent protein (GFP) (4×105 cells/5µl PBS) were injected at a rate of 0.5µl/min into the right bregma of nude rats at a distance of 3mm. On the 21st day after tumor cell injection, Cilengitide (4mg/kg) was intraperitoneally injected, and the rats were sacrificed 48 hours later and the brain tissues were removed. The brain tissues were fixed with 10% formalin overnight and placed in a coronal brain tissue slide box, then cut into 2mm thick sections. The 2mm sections containing tumors were frozen in optimal cutting temperature (OCT) tissue blocks and subjected to autophagy-related immunofluorescence analysis. |
Dosage form | 4mg/kg for once; i.p. |
Applications | Cilengitide significantly induced autophagy in the xenograft tumors of rat. |
References: | |
| Cas No. | 188968-51-6 | SDF | |
| Überlieferungen | EMD 121974 | ||
| Chemical Name | 2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid | ||
| Canonical SMILES | CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N | ||
| Formula | C27H40N8O7 | M.Wt | 588.66 |
| Löslichkeit | ≥ 29.433mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6988 mL | 8.4939 mL | 16.9877 mL |
| 5 mM | 339.8 μL | 1.6988 mL | 3.3975 mL |
| 10 mM | 169.9 μL | 849.4 μL | 1.6988 mL |
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Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)