Cilengitide(Synonyms: 西仑吉肽; EMD 121974)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Cilengitide (Synonyms: 西仑吉肽; EMD 121974) 纯度: 99.30%

Cilengitide (EMD 121974) 是一种有效的选择性整合素 ανβ3 和 ανβ5 抑制剂。Cilengitide 抑制 ανβ3 和 ανβ5 与玻连蛋白结合，IC50 值分别为 4 和 79 nM。

Cilengitide(Synonyms: 西仑吉肽; EMD 121974)

Cilengitide Chemical Structure

CAS No. : 188968-51-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1590 In-stock
5 mg ￥1228 In-stock
10 mg ￥1739 In-stock
50 mg ￥5500 In-stock
100 mg ￥8500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Cilengitide 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • CNS-Penetrant Compound Library
  • Autophagy Compound Library
  • Drug Repurposing Compound Library
  • Macrocyclic Compound Library
  • Anti-COVID-19 Compound Library
  • Cytoskeleton Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Targeted Diversity Library
  • Rare Diseases Drug Library

生物活性

Cilengitide (EMD 121974) is a potent and selective inhibitor of the integrins ανβ3 and ανβ5. Cilengitide inhibits binding of isolated ανβ3 and ανβ5 to Vitronectin with an IC50 value of 4 and 79 nM, respectively [1].

IC50 & Target[1]

αvβ3

4 nM (IC50, Binds to Vitronectin)

αvβ5

79 nM (IC50, Binds to Vitronectin)

体外研究
(In Vitro)

Cilengitide is a cyclized RGD (Arg-Gly-Asp motif)-containing pentapeptide. Cilengitide blocks integrin ανβ3- and ανβ5-mediated endothelial cell attachment and migration[1].
Cilengitide inhibits integrin-mediated binding to Vitronectin with IC50‘s of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines [1].
Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC50 of 2 μM [1].

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.
体内研究
(In Vivo)

Cilengitide (i.p. at 10, 50, and 250 μg three times per week) inhibits M21-L melanoma tumors growth in nude mice [1].

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.

Animal Model: Nude mice bearing M21-L melanoma tumors[1]
Dosage: 10, 50, and 250 μg
Administration: Dosed i.p. three times per week
Result: Demonstrated 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.

Clinical Trial

分子量

588.66

Formula

C27H40N8O7
CAS 号

188968-51-6
中文名称

西仑吉肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 100 mg/mL (169.88 mM; Need ultrasonic)

DMSO : ≥ 44 mg/mL (74.75 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6988 mL 8.4939 mL 16.9877 mL
5 mM 0.3398 mL 1.6988 mL 3.3975 mL
10 mM 0.1699 mL 0.8494 mL 1.6988 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务