Cilengitide TFA (EMD 121974)

Alias: EMD 121974; NSC-707544;EMD-85189;D-03497; EMD-121974; EMD121974; NSC 707544; EMD 85189; NSC707544;EMD85189; D03497;D 03497
Cat No.:V1596 Purity: ≥98%
Cilengitide TFA (also known as EMD 121974;NSC-707544;EMD-85189;D-03497), the trifluoroacetic acid salt of cilengitide, is a highly potent and selective integrin inhibitor for the αvβ3 receptor and the αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; it showed~10-fold selectivity against gpIIbIIIa.
Cilengitide TFA (EMD 121974) Chemical Structure CAS No.: 199807-35-7
Product category: Integrin
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Cilengitide TFA (EMD 121974):

  • Cilengitide (EMD 121974)
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Top Publications Citing lnvivochem Products
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cilengitide TFA (also known as EMD 121974; NSC-707544; EMD-85189; D-03497), the trifluoroacetic acid salt of cilengitide, is a highly potent and selective integrin inhibitor for the αvβ3 receptor and the αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; it showed ~10-fold selectivity against gpIIbIIIa. Cilengitide is a cyclic Arg-Gly-Asp based peptide with potential antineoplastic activity and has been extensively studied for its anticancer application. The mechanism of action for cilengitide is to bind to and inhibit the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. Cilengitide is currently undergoing phase 2 clinical trials, and the European Medicines Agency has granted cilengitide orphan drug status.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
An antagonist of the αvβ3 and αvβ5 integrin receptor is cilengitide (EMD 121974). In investigations assessing cell adhesion in human lung cancer cell lines UCLA-P3 or melanoma M21, respectively, clengitide reduced integrin-mediated binding to vitronectin with an IC50 of 0.4 and 0.4 μM [1]. In vitro, cilengitide demonstrates concentration- and time-dependent cytotoxic effects at concentrations higher than 1 μM [2].
ln Vivo
Cilenegitide (10, 50, and 250 μg) was injected intraperitoneally three times a week into nude mice with M21-L melanoma tumors; the doses were demonstrated to suppress tumor growth and concurrently reduce tumor volume (55%, 75%, and 55%, respectively). Tumor weight (23%, 38%, and 61%, respectively) and 89% [2]. ILP administered with cilengitide alone, ILP administered with cilengitide plus melphalan, TNF, or both did not influence the systemic pharmacokinetics of cilengitide administered intraperitoneally in the rat model under study. After 10 minutes of intraperitoneal treatment, systemic levels of cilengitide reach about 20 μg/mL (about 35 μM) and keep rising to about 40 μg/mL (about 70 μM) within the first hour. After then, there is a 2.1-hour elimination half-life for serum levels of celibitide [3].
Animal Protocol
Dissolved in PBS; 100μg; i.p. injection
Human glioblastoma xenografts U87 MG
References
[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 TL, et al. The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model. Int J Cancer. 2012 Nov 13
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H41F3N8O9
Molecular Weight
702.68
CAS #
199807-35-7
SMILES
FC(C(=O)O)(F)F.O=C1[C@H](C(C)C)N(C)C([C@@H](CC2C=CC=CC=2)NC([C@H](CC(=O)O)NC(CNC([C@H](CCC/N=C(\N)/N)N1)=O)=O)=O)=O
Synonyms
EMD 121974; NSC-707544;EMD-85189;D-03497; EMD-121974; EMD121974; NSC 707544; EMD 85189; NSC707544;EMD85189; D03497;D 03497
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (142.3 mM)
Water: 8 mg/mL (11.4 mM)
Ethanol:<1 mg/mL
Solubility (In Vivo)
30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.4231 mL 7.1156 mL 14.2312 mL
5 mM 0.2846 mL 1.4231 mL 2.8462 mL
10 mM 0.1423 mL 0.7116 mL 1.4231 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
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