Home Cytoskeletal Signaling Integrin inhibitor Cilengitide For research use only.

Cilengitide

Synonyms: EMD 121974, EMD-12192, EMD-85189, NSC-​707544

Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-​707544) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5 with IC50 of 4 and 79 nM, respectively.

Cilengitide Chemical Structure

Cilengitide Chemical Structure

CAS: 188968-51-6

Selleck's Cilengitide has been cited by 36 publications

Purity & Quality Control

Batch: Purity: 99.63%
99.63

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Biological Activity

Description Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-​707544) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5 with IC50 of 4 and 79 nM, respectively.
Targets
integrin ανβ3 [1]
(Cell-free assay)		 integrin ανβ5 [1]
(Cell-free assay)
4 nM 79 nM
In vitro
In vitro

Cilengitide inhibits a receptor reported to activate KRAS named ITGAV. [2]
Cell Research Cell lines MCF10A, HuMEC cells
Concentrations 10 μM
Incubation Time 1 h
Method

MCF10A and HuMEC cells were plated at the center of wells in 6-well plates. 24 hours after plating, colonies were washed with PBS and cells were pretreated for 1 hour in media with or without 1 μM U0126, 1 μM LY294002, 100 nM erlotinib, 1 μM crizotinib, 1 μM infigratininb or 10 μM cilengitide. After pre-incubation, medium was replaced with medium with or without 4 ng/ml TGF-β1 as well as any inhibitor with which cells were pretreated. TGF-β1 was replenished every 48 hours. After 7 days, samples were harvested and processed for flow cytometry of EMT marker protein levels as described above.

(Data sourced from selleck products)

Chemical Information & Solubility

Molecular Weight 588.66 Formula

C27H40N8O7
CAS No. 188968-51-6 SDF --
Smiles CC(C)C1N(C)C(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(O)=O)NC(=O)CNC(=O)C(CCCNC(N)=N)NC1=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (169.87 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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