IF 14
PMID: 42468382 ↗Cilengitide
Catalog No.: GC13559Purity:>99.00%Synonyms: EMD 121974
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.
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Cas No.: 188968-51-6
10mM (in 1mL DMSO)In Stock
$128.00
1
5mgIn Stock
$94.00
1
10mgIn Stock
$142.00
1
25mgIn Stock
$246.00
1
50mgIn Stock
$410.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $128.00 | In Stock | 1 | |
| 5mg | $94.00 | In Stock | 1 | |
| 10mg | $142.00 | In Stock | 1 | |
| 25mg | $246.00 | In Stock | 1 | |
| 50mg | $410.00 | In Stock | 1 |
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Zitate (Citations)
1 publicationsPublikationen von Forschern, die dieses Produkt verwendenBeschreibung (Description)
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.
Protokoll (Protocol)
| 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: | |
Produktdokumente (Product Documents)
Purity:>99.00%Appearance:A solid
Chemische Eigenschaften (Chemical Properties)
CAS-Nr.
188968-51-6
Synonyme
EMD 121974
Chemischer 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
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
Summenformel
C27H40N8O7
Molekulargewicht
588.66
Löslichkeit
≥ 29.433mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.
Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit
g/mol
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