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Cilengitide TFA (Synonyms: EMD 121974 TFA) 纯度: 98.85%
Cilengitide 是有效的,选择性的 αvβ3 和 αvβ5 受体整合素抑制剂,IC50 分别为 4 nM 和 79 nM。
Cilengitide TFA Chemical Structure
CAS No. : 199807-35-7
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in Water | ¥2320 | In-stock | |
5 mg | ¥1500 | In-stock | |
10 mg | ¥2500 | In-stock | |
25 mg | ¥4500 | In-stock | |
50 mg | 询价 | ||
100 mg | 询价 |
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生物活性 |
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively. |
IC50 & Target |
IC50: 4/79 nM (αvβ3/αvβ5)[1]. |
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体外研究 (In Vitro) |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
702.68 |
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Formula |
C29H41F3N8O9 |
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CAS 号 |
199807-35-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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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) |
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溶解性数据 |
In Vitro:
H2O : 25 mg/mL (35.58 mM; Need ultrasonic) 配制储备液
*
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。 |
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参考文献 |
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Cell Assay [2] |
The cytotoxicity of the two drugs, Belotecan and Cilengitide, is measured by the Cell Counting Kit-8 (CCK-8). U87MG and U251MG cells are seeded in 96 well plates at a density of 4×103 cells per well to allow for adhesion overnight. After this, the cells are treated with Cilengitide at a concentration of 0, 0.1, 0.5, 1, 5 and 25 µM and Belotecan at a concentration of 0, 6.25, 12.5, 25, 50 and 100 nM. All possible combinations of concentrations are used to assess the combined therapeutic effect of Cilengitide and Belotecan. After 3 days, 10 µL of the CCK-8 solution is added to each well of the plate, and the plate is incubated for 3 hr in the incubator (37°C; 5% CO2)[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [2][3] |
Mice[2] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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