Cilengitide TFA

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Cilengitide TFA

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

199807-35-7

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品名称

EMD 121974 TFA

产品介绍

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。

生物活性

Cilengitide is a potent and selectiveintegrininhibitor for α_vβ₃and α_vβ₅receptor, withIC₅₀values of 4 nM and 79 nM, respectively.

IC₅₀& Target

IC50: 4/79 nM (α_vβ₃/α_vβ₅)^[1].

体外研究
(In Vitro)

Cilengitide (EMD 121974) is the α_vβ₃and α_vβ₅integrin 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].

体内研究
(In Vivo)

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].

Clinical Trial

分子量

702.68

性状

Solid

Formula

C₂₉H₄₁F₃N₈O₉

CAS 号

199807-35-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

溶解性数据

In Vitro:

H₂O : 25 mg/mL(35.58 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 16.67 mg/mL (23.72 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。