Cilengitide

• 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

• Clinical Information:

  Phase 3

• CAS Number:

  188968-51-6