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Cilengitide

Catalog No. T2494 CAS 188968-51-6

Synonyms: EMD 121974

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.

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Cilengitide, CAS 188968-51-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 45.00
2 mg	In stock	$ 64.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 163.00
25 mg	In stock	$ 288.00
50 mg	In stock	$ 463.00
100 mg	In stock	$ 666.00
1 mL * 10 mM (in DMSO)	In stock	$ 139.00

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Purity: 99.8%

Purity: 99.36%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays); ~10-fold selectivity against gpIIbIIIa.
Targets&IC50	αvβ5:79 nM, αvβ3:4.1nM
Cell Research	Cilengitide is supplied as an apyrogenic sterile infusion solution in physiological saline. Cilengitide is diluted in saline to a concentration of 1 mM[2]. The cytotoxicity of the two drugs, Belotecan and Cilengitide, is measured by the Cell Counting Kit-8 (CCK-8). U87 mg and U251 mg cells are seeded in 96 well plates at a density of 4×103 cells per well to allow for adhesion overnight. After this, the cells are treated with Cilengitide at a concentration of 0, 0.1, 0.5, 1, 5 and 25 μM and Belotecan at a concentration of 0, 6.25, 12.5, 25, 50 and 100 nM. All possible combinations of concentrations are used to assess the combined therapeutic effect of Cilengitide and Belotecan. After 3 days, 10 μL of the CCK-8 solution is added to each well of the plate, and the plate is incubated for 3 hr in the incubator (37°C; 5% CO2). The optical density (OD) of the sample plate is measured at 450 nm in a microplate reader. The viability of tumor cells is assessed by calculating the OD ratio of the specific OD in each sample to that of the control. Each experiment is conducted in quadruplicate. The values are averaged and normalized against the controls to generate dose-response curves[2].

Synonyms	EMD 121974
Molecular Weight	588.66
Formula	C27H40N8O7
CAS No.	188968-51-6

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 32 mg/mL

DMSO: 44 mg/mL

References and Literature

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. Kim YH, et al. Combination therapy of cilengitide with belotecan against experimental glioblastoma. Int J Cancer. 2013 Aug 1;133(3):749-56. 3. ten Hagen, T., Seynhaeve, A., de Wiel-Ambagtsheer, G., de Bruijn, E., van Tiel, S., & Ruegg, C. et al. (2012). The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model. International Journal Of Cancer, 132(11), 2694-2704. doi: 10.1002/ijc.27940

Citations

1. Xing Q, Feng Y, Sun H, et al. Scavenger receptor MARCO contributes to macrophage phagocytosis and clearance of tumor cells. Experimental Cell Research. 2021: 112862

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Peptide Compound Library Human Metabolite Library Pediatric Drug Library Macrocyclic Compound Library ReFRAME Related Library Anti-Lung Cancer Compound Library

Related Products

Related compounds with same targets

mP6 BIO-1211 CWHM-12 Roxifiban acetate αvβ6 integrin inhibitor 2 GRGDSP acetate(91037-75-1 free base) Gly-Arg-Gly-Asp-Ser acetate(96426-21-0 free base) RGD

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Keywords

Cilengitide 188968-51-6 Autophagy Cytoskeletal Signaling Integrin Inhibitor EMD121974 ανβ5 ανβ3 integrins Vitronectin EMD-121974 inhibit EMD 121974 inhibitor

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