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Cilengitide TFA (Synonyms: EMD 121974 TFA)

Catalog No.GC61520

Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.

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Cilengitide TFA Chemical Structure

Cas No.: 199807-35-7

Size Price Stock Qty
10mM (in 1mL Water)
$125.00
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5mg
$81.00
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10mg
$135.00
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25mg
$261.00
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50mg
$405.00
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100mg
$630.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.

Cilengitide (EMD 121974) is the αvβ3 and αvβ5 integrin receptor antagonist. In cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines, Cilengitide inhibits integrin-mediated binding to vitronectin with IC50s of 0.4 and 0.4 μM[1]. In vitro treatment of Cilengitide, at a concentration greater than 1 µM, shows concentration- and time-dependent cytotoxic effects [2].

In nude mice bearing M21-L melanoma tumors, Cilengitide dose i.p. at 10, 50, and 250 μg three times per week demonstrate 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[2]. In the rat model studied, the systemic pharmacokinetics of i.p. Cilengitide are not affected by ILP with Cilengitide alone or ILP with Cilengitide plus Melphalan, TNF or both. Systemic Cilengitide levels reach around 20 µg/mL (approximately 35 µM) within 10 min of i.p. administration and continued to rise to approximately 40 µg/mL (approximately 70 µM) in the first hour. Thereafter Cilengitide levels in serum drop with an elimination half-life of 2.1 hr[3].

[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.

Chemical Properties

Cas No. 199807-35-7 SDF
Synonyms EMD 121974 TFA
Canonical 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.FC(F)(C(O)=O)F
Formula C29H41F3N8O9 M.Wt 702.68
Solubility Water: 25 mg/mL (35.58 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Reviews

Review for Cilengitide TFA

Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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