Cilengitide (Synonyms: EMD 121974)

Name: Cilengitide
Brand: MedChemExpress
SKU: HY-16141
Rating: 5.0 (49 reviews)

Cat. No.: HY-16141 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

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Cilengitide (EMD 121974) is a potent integrins antagonist with IC₅₀s of 0.61 nM (α_νβ₃), 8.4 nM (α_νβ₅) and 14.9 nM (α₅β₁), respectively. Cilengitide inhibits the binding of α_νβ₃ and α_νβ₅ 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.

For research use only. We do not sell to patients.

Cilengitide Chemical Structure

CAS No. : 188968-51-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 171	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 171	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 224	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 740	In-stock	Estimated Time of Arrival: December 31
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Based on 49 publication(s) in Google Scholar

Other Forms of Cilengitide:

Cilengitide TFA Get quote

43 Publications Citing Use of MCE Cilengitide

Proliferation Assay

IHC

: Cilengitide purchased from MedChemExpress. Usage Cited in: Cell Adh Migr. 2019 Jan 21:1-12. [Abstract]; HepG2 cells are loaded with FSS at 1 dyn/cm2 for 0.5 h, with or without treatment of 0.5 μM Cli for 6 h prior to FSS application. Lysates are probed with antibodies as indicated.

: Cilengitide purchased from MedChemExpress. Usage Cited in: J Transl Med. 2018 Dec 12;16(1):352. [Abstract]; Representative images of immunofluorescence performed for α-SMA on WKY- and SHR-CF in the treatment of TGF-β1, cilengitide or both.

: Cilengitide purchased from MedChemExpress. Usage Cited in: J Transl Med. 2018 Dec 12;16(1):352. [Abstract]; Representative Western blot images of ανβ5 and collagen I protein expression in WKY- and SHR-CF cultured on substrates with two different stiffness (high and low) and contemporary treated with 5 ng/ml TGF-β1, TGF-β1 + 0.5 μM cilengitide, or cilengitide.

: Cilengitide purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2018 Apr 1;314(4):C415-C427. [Abstract]; C2C12 cells are pre-incubated with different concentrations of Cilengitide prior to LPA 20 μg/mL addition and incubation for 3 hours. CTGF levels are analyzed.

: Cilengitide purchased from MedChemExpress. Usage Cited in: PLoS One. 2016 Feb 3;11(2):e0148333. [Abstract]; Blockade of cellular adhesion of HEK 293 cells at 10 or 30 nM coated recombinant OPN forms with 1μM antagonistic integrin inhibitors. RGES (black bars) is used as a control peptide. Cilengitide (white bars) inhibits the integrins α_Vβ₃, α_Vβ₅, and α₅β₁. TR-14035 (hatched bars) inhibits the integrins α₄β₇ and α₄β₁. Depicted are the means ± SEM of 3 independent experiments. * indicate signif

: Cilengitide purchased from MedChemExpress. Usage Cited in: Department of Bioengineering. Santa Clara University. Jun 12, 2014 .; Cilengitide Photos: Pictures of migration through alginate with and without Cilengitide after four days. A) The view of the bottom of the untreated well, showing a healthy monolayer of U87s. B) The view of the cells suspended in alginate in the untreated well. A few of the multiple migrated cells within the image are marked with arrows. C) The view of the bottom of the Cilengitide treated well, showing very few, ill-attached U87s. D). The view of cells suspended in alginate in the Cilengitide-tr

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]^[3]

αvβ3

4 nM (IC₅₀, αvβ3-Vitronectin interaction^[2])

αvβ5

79 nM (IC₅₀, αvβ5-Vitronectin interaction^[2])

αvβ3

0.61 nM (IC₅₀, ^[1])

αvβ5

8.4 nM (IC₅₀, ^[1])

α5β1

14.9 nM (IC₅₀, ^[1])

STAT3

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.54 nM Compound: Cilengitide	Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta3 (Gly27 to Asp718 residues) expressed in CHO cells by ELISA based solid phase binding assay	[PMID: 32094009]
CHO	IC₅₀	15.4 nM Compound: Cilengitide	Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay Inhibition of fibronectin binding to recombinant human integrin alpha5 (Phe42 to Tyr995 residues) beta1 (Gln21 to Asp728 residues) expressed in CHO cells by ELISA based solid phase binding assay	[PMID: 32094009]
CHO	IC₅₀	8 nM Compound: Cilengitide	Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay Inhibition of vitronectin binding to recombinant human integrin alphaV (Phe31 to Val992 residues) beta5 (Gly24 to Asn719 residues) expressed in CHO cells by ELISA based solid phase binding assay	[PMID: 32094009]
HEK-293T	IC₅₀	0.51 nM Compound: c(RGDfV)	Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay	[PMID: 24095096]
M21	IC₅₀	0.4 nM Compound: c[RGDf(Me)V]; Cilengitide	Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2 Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2	[PMID: 26753814]

In Vitro

Cilengitide is a cyclized RGD (Arg-Gly-Asp motif)-containing pentapeptide. Cilengitide blocks integrin ανβ3- and ανβ5-mediated endothelial cell attachment and migration^[2].
Cilengitide inhibits integrin-mediated binding to Vitronectin with IC₅₀s of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines^[2].
Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC₅₀ of 2 μM^[2].
Cilengitide (0-1 mg/mL; 24-72 h) inhibits cell viability of melanoma cells in vitro and (5 μg/mL; 12 h) induces B16 and A375 cells apoptosis^[3].
Cilengitide (5 μg/mL, 10 μg/mL; 2 weeks) inhibits colony formation of B16 and A375 cells^[3].
Cilengitide (0-20 μg/mL; 12 h) inhibits STAT3 phosphorylation to decrease the expression of PD-L1^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[3]

Cell Line:	B16 and A375 cells
Concentration:	0, 5, 10, and 20 μg/mL
Incubation Time:	12 hours
Result:	Suppressed PD-L1 expression and STAT3 phosphorylation at concentrations greater than 5 µg/mL.

Apoptosis Analysis^[3]

Cell Line:	B16 and A375 cells
Concentration:	5 μg/mL
Incubation Time:	12 hours
Result:	Resulted apoptosis rates in B16 and A375 cells of 15.27% and 14.89%, respectively.

In Vivo

Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice^[2].
Cilengitide (50 mg/kg; i.p.; daily) enhances the function of CD8+ T cells and promotes anti-PD1 efficacy with Anti-PD1 monoclonal antibody in B16 murine melanoma model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing M21-L melanoma tumors^[2]
Dosage:	10, 50, and 250 μg
Administration:	Dosed i.p. three times per week
Result:	Demonstrated inhibition of tumor growth with a reduction in both tumor volume (55%, 75%, and 89%, respectively) and tumor weight (23%, 38%, and 61%, respectively), when compared to controls.

Animal Model:	Female C57BL/6 mice (6-8 weeks old) with B16 cells s.c.^[3]
Dosage:	50 mg/kg; with or without 10 mg/kg Anti-PD1 monoclonal antibody or isotype control i.p. every 3 days;
Administration:	Intraperitoneal injection; daily
Result:	Downregulated the expression of PD-L1 via STAT3 pathway and decreased the expression of PD-L1.

Clinical Trial

Molecular Weight

588.66

Formula

C₂₇H₄₀N₈O₇

CAS No.

188968-51-6

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (169.88 mM; Need ultrasonic)

DMSO : ≥ 44 mg/mL (74.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6988 mL	8.4939 mL	16.9877 mL
5 mM	0.3398 mL	1.6988 mL	3.3975 mL
10 mM	0.1699 mL	0.8494 mL	1.6988 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (169.88 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.80%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (253 KB) HNMR (312 KB) LCMS (86 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.6988 mL	8.4939 mL	16.9877 mL	42.4693 mL
	5 mM	0.3398 mL	1.6988 mL	3.3975 mL	8.4939 mL
	10 mM	0.1699 mL	0.8494 mL	1.6988 mL	4.2469 mL
	15 mM	0.1133 mL	0.5663 mL	1.1325 mL	2.8313 mL
	20 mM	0.0849 mL	0.4247 mL	0.8494 mL	2.1235 mL
	25 mM	0.0680 mL	0.3398 mL	0.6795 mL	1.6988 mL
	30 mM	0.0566 mL	0.2831 mL	0.5663 mL	1.4156 mL
	40 mM	0.0425 mL	0.2123 mL	0.4247 mL	1.0617 mL
	50 mM	0.0340 mL	0.1699 mL	0.3398 mL	0.8494 mL
	60 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL
H₂O	80 mM	0.0212 mL	0.1062 mL	0.2123 mL	0.5309 mL
H₂O	100 mM	0.0170 mL	0.0849 mL	0.1699 mL	0.4247 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Cilengitide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cilengitide188968-51-6EMD 121974EMD121974EMD-121974IntegrinAutophagyApoptosisSTATPD-1/PD-L1PD-1/Programmed death-ligand 1integrinsανβ3ανβ5VitronectinInhibitorinhibitorinhibit

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Cilengitide (Synonyms: EMD 121974)

Customer Review

Other Forms of Cilengitide:

Cilengitide Related Antibodies

43 Publications Citing Use of MCE Cilengitide

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•Related Screening Libraries:

•Related Small Molecules:

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View All Integrin Isoform Specific Products:

View All STAT Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cilengitide Related Antibodies

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Complete Stock Solution Preparation Table

Cilengitide Related Classifications

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