Cilengitide 是有效的，选择性的 α_vβ₃ 和 α_vβ₅ 受体整合素抑制剂，IC₅₀ 分别为 4 nM 和 79 nM。

Cilengitide is a potent and selective integrin inhibitor for α v β 3 and α v β 5 receptor, with IC 50 values of 4 nM and 79 nM, respectively.

Solid

IC50: 4/79 nM (αvβ3/αvβ5).

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. In vitro treatment of Cilengitide, at a concentration greater than 1 μM, shows concentration- and time-dependent cytotoxic effects . has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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. has not independently confirmed the accuracy of these methods. They are f

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: H₂O : 25 mg/mL (35.58 mM; Need ultrasonic)配制储备液