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Cilengitide Integrin inhibitor

Cat.No.S6387

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 Integrin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 588.66

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 588.66 Formula

C27H40N8O7

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 188968-51-6 -- Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (169.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 5 mg/mL (超声加热十分钟,60℃)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
integrin ανβ3 [1]
(Cell-free assay)
4 nM
integrin ανβ5 [1]
(Cell-free assay)
79 nM
In vitro

Cilengitide inhibits a receptor reported to activate KRAS named ITGAV. [2]

References

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