Cilengitide

Catalog No.S6387 Batch:S638701

Technical Data

Formula	C₂₇H₄₀N₈O₇
Molecular Weight	588.66	CAS No.	188968-51-6
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (169.87 mM)
		Water	100 mg/mL (169.87 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) is a potent and selective inhibitor of the integrins α_νβ₃ and α_νβ₅ with IC50 of 4 and 79 nM, respectively.

Targets

integrin α_νβ₃ ^[1] (Cell-free assay)	integrin α_νβ₅ ^[1] (Cell-free assay)
4 nM	79 nM

In vitro

Cilengitide inhibits a receptor reported to activate KRAS named ITGAV. ^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines MCF10A, HuMEC cells Concentrations 10 μM Incubation Time 1 h Method MCF10A and HuMEC cells were plated at the center of wells in 6-well plates. 24 hours after plating, colonies were washed with PBS and cells were pretreated for 1 hour in media with or without 1 μM U0126, 1 μM LY294002, 100 nM erlotinib, 1 μM crizotinib, 1 μM infigratininb or 10 μM cilengitide. After pre-incubation, medium was replaced with medium with or without 4 ng/ml TGF-β1 as well as any inhibitor with which cells were pretreated. TGF-β1 was replenished every 48 hours. After 7 days, samples were harvested and processed for flow cytometry of EMT marker protein levels as described above. (Data sourced from selleck products)
Animal Study:^{^[1]}	Animal Models Nude mice Dosages 10, 50, and 250 µg Administration i.p.

Cell Assay:^{^[2]}

Cell lines
MCF10A, HuMEC cells
Concentrations
10 μM
Incubation Time
1 h
Method
MCF10A and HuMEC cells were plated at the center of wells in 6-well plates. 24 hours after plating, colonies were washed with PBS and cells were pretreated for 1 hour in media with or without 1 μM U0126, 1 μM LY294002, 100 nM erlotinib, 1 μM crizotinib, 1 μM infigratininb or 10 μM cilengitide. After pre-incubation, medium was replaced with medium with or without 4 ng/ml TGF-β1 as well as any inhibitor with which cells were pretreated. TGF-β1 was replenished every 48 hours. After 7 days, samples were harvested and processed for flow cytometry of EMT marker protein levels as described above.

(Data sourced from selleck products)

Animal Study:^{^[1]}

Animal Models
Nude mice
Dosages
10, 50, and 250 µg
Administration
i.p.

References

Selleck's Cilengitide has been cited by 37 publications

hUC-MSCs-derived MFGE8 ameliorates locomotor dysfunction via inhibition of ITGB3/ NF-κB signaling in an NMO mouse model [ NPJ Regen Med, 2024, 9(1):4]	PubMed: 38242900
Milk fat globule epidermal growth factor 8 alleviates liver injury in severe acute pancreatitis by restoring autophagy flux and inhibiting ferroptosis in hepatocytes [ World J Gastroenterol, 2024, 30(7):728-741]	PubMed: 38515944
Tissue factor is a critical regulator of radiation therapy-induced glioblastoma remodeling [ Cancer Cell, 2023, 41(8):1480-1497.e9]	PubMed: 37451272
Self-generated gradients steer collective migration on viscoelastic collagen networks [ Nat Mater, 2022, 10.1038/s41563-022-01259-5]	PubMed: 35637338
Developmental endothelial locus-1 protects from hypertension-induced cardiovascular remodeling via immunomodulation [ J Clin Invest, 2022, e126155]	PubMed: 35133978
Integrin β3-PKM2 pathway-mediated aerobic glycolysis contributes to mechanical ventilation-induced pulmonary fibrosis [ Theranostics, 2022, 12(14):6057-6068]	PubMed: 36168620
Fibroblast growth factor receptor 4 promotes glioblastoma progression: a central role of integrin-mediated cell invasiveness [ Acta Neuropathol Commun, 2022, 10(1):65]	PubMed: 35484633
Macrophage-like THP-1 Cells Derived from High-Density Cell Culture Are Resistant to TRAIL-Induced Cell Death via Down-Regulation of Death-Receptors DR4 and DR5 [ Biomolecules, 2022, 12(2)150]	PubMed: 35204655
Cell clusters adopt a collective amoeboid mode of migration in confined nonadhesive environments [ Sci Adv, 2022, 8(39):eabp8416]	PubMed: 36179021
Cyr61 from adipose-derived stem cells promotes colorectal cancer metastasis and vasculogenic mimicry formation via integrin αV β5 [ Mol Oncol, 2021, 15(12):3447-3467]	PubMed: 33999512

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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