Cilengitide
Product Specifications
UNSPSC Description
Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers[1][2][3].
Target Antigen
Apoptosis; Autophagy; Integrin; PD-1/PD-L1; STAT
Type
Reference compound
Related Pathways
Apoptosis;Autophagy;Cytoskeleton;Immunology/Inflammation;JAK/STAT Signaling;Stem Cell/Wnt
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Cilengitide.html
Solubility
DMSO : ≥ 44 mg/mL|H2O : 100 mg/mL (ultrasonic)
Smiles
O=C(NCC(N[C@H](C(N[C@H](CC1=CC=CC=C1)C(N([C@H]2C(C)C)C)=O)=O)CC(O)=O)=O)[C@H](CCCNC(N)=N)NC2=O
Molecular Weight
588.66
References & Citations
[1]Hariharan S, et al. Assessment of the biological and pharmacological effects of the alpha nu beta3 and alpha nu beta5 integrinreceptor antagonist, Cilengitide (EMD 121974), in patients with advanced solid tumors. Ann Oncol. 2007 Aug;18(8):1400-7.|[2]Kapp TG, et al. A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins. Sci Rep. 2017 Jan 11;7:39805. |[3]Pan X, et al. Cilengitide, an αvβ3-integrin inhibitor, enhances the efficacy of anti-programmed cell death-1 therapy in a murine melanoma model. Bioengineered. 2022 Feb;13(2):4557-4572.
Shipping Conditions
Blue Ice
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-16141/Cilengitide-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-16141/Cilengitide-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
188968-51-6
Available Sizes
Curated Selection
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