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Cilengitide

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].

Product Specifications

CAS Number

[188968-51-6]

Product Name Alternative

EMD 121974

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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

Purity

99.91

Solubility

DMSO : ≥ 44 mg/mL|H2O : 35 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 Formula

C27H40N8O7

Molecular Weight

588.66

Precautions

H302, H315, H319, H335

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

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

STAT3; α5β1; αvβ3; αvβ5

Citation 01

Adv Sci (Weinh) . 2025 Apr 28:e2504647.|Adv Sci (Weinh) . 2025 Oct 30:e01602.|Am J Physiol Cell Physiol. 2018 Apr 1;314 (4) :C415-C427.|Atheroscler Plus. 2022 Oct 19:50:57-64.|Biochim Biophys Acta Mol Basis Dis. 2024 Aug 31:167484.|Bioengineered. 2022 Feb;13 (2) :4557-4572.|Biomed Res Int. 2021 Nov 30:2021:5954757.|bioRxiv. 2020 Apr.|bioRxiv. 2024 Aug 28:2024.08.27.609975.|bioRxiv. 2025 Sep 21.|Blood Rev. 2023 May:59:101038.|Br J Cancer. 2023 Mar;128 (7) :1344-1359.|Cancer Cell. 2021 Nov 8;39 (11) :1531-1547.e10.|Cancer Med. 2018 Feb;7 (2) :408-419. |Cancers (Basel) . 2023 Mar 12;15 (6) :1729.|Cell Adh Migr. 2019 Dec;13 (1) :152-163.|Cell Biol Int. 2020 Apr;44 (4) :966-974.|Cell Death Dis. 2022 Dec 7;13 (12) :1028.|Cell Rep Med. 2025 Jan 16:101922.|Cell Rep. 2022 Sep 27;40 (13) :111422.|Cell. 2020 Aug 6;182 (3) :545-562.e23. |Clin Transl Med. 2021 Oct;11 (10) :e548.|Commun Biol. 2024 Dec 30;7 (1) :1713.|Department of Bioengineering. Santa Clara University. Jun 12, 2014 .|Engineering. 8 October 2020.|Environ Pollut. 2023 Aug 1:330:121817.|FASEB J. 2023 Feb;37 (2) :e22726.|Free Radic Biol Med. 2024 Dec 9:227:296-311.|Front Immunol. 2018 Jun 1:9:1207.|Front Pharmacol. 2021 Feb 24:12:585778.|Int Immunopharmacol. 2024 Jul 1:138:112545.|Int J Biol Sci. 2025 May 27;21 (8) :3573-3596.|J Cell Biol. 2023 Aug 7;222 (8) :e202303107.|J Cell Physiol. 2024 Jun;239 (6) :e31267.|J Chem Inf Model. 2023 Oct 23;63 (20) :6302-6315.|J Clin Invest. 2025 Oct 16:e188822.|J Immunother Cancer. 2020 Mar;8 (1) :e000111. |J Integr Neurosci. 2024 Jul 25;23 (7) :140.|J Mol Histol. 2020 Apr;51 (2) :147-159.|J Oral Pathol Med. 2025 Aug;54 (7) :597-606.|J Transl Med. 2018 Dec 12;16 (1) :352.|J Vis Exp. 2025 May 23: (219) .|Lung. 2020 Dec;198 (6) :947-955.|medRxiv. 2025 Mar 23.|Mol Cancer Ther. 2022 Sep 6;21 (9) :1485-1496.|Mol Cell Biochem. 2025 Oct 20.|Nat Cell Biol. 2020 Mar;22 (3) :289-296. |Nat Mater. 2025 Sep 1.|Obesity. 2015 Apr;23 (4) :779-85. |Oncogene. 2025 Jul;44 (28) :2396-2412.|Oncoimmunology. 2025 Dec;14 (1) :2508057.|Patent. US20180263995A1.|Patent. US20220378739A1.|PLoS One. 2014 Oct 13;9 (10) :e110453.|PLoS One. 2016 Feb 3;11 (2) :e0148333. |Research Square Preprint. 2022 Jan.|Respir Res. 2025 Jul 2;26 (1) :229.|Scand Cardiovasc J. 2021 Oct;55 (5) :287-296.|SSRN. 2025 Feb 19.|SSRN. 2025 Jul 7.|Stem Cell Reports. 2017 Dec 12;9 (6) :1948-1960.|Biochem Pharmacol. 2025 Jun:236:116870.|Cell Mol Gastroenterol Hepatol. 2025 May 29:101548.

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