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Cilengitide
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。
Cilengitide图片
CAS NO:188968-51-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
西仑吉肽
EMD 121974
产品介绍
Cilengitide (EMD 121974) 是一种强效的整合素拮抗剂,IC50分别为 0.61 nM (ανβ3),8.4 nM (ανβ5) 和 14.9 nM (α5β1)。Cilengitide 抑制ανβ3ανβ5与玻连蛋白结合,IC50值分别为 4 和 79 nM。Cilengitide 能够抑制TGF-β/Smad信号通路,调节PD-L1表达。Cilengitide 诱导凋亡 (apoptosis),在对胶质母细胞瘤和其他癌症的研究中也显示出抗血管生成的作用。
生物活性

Cilengitide (EMD 121974) is a potentintegrinsantagonist withIC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding ofανβ3andανβ5to Vitronectin withIC50s of 4 nM and 79 nM, respectively. Cilengitide inhibitsTGF-β/Smadsignaling, mediatesPD-L1expression. Cilengitide also inducesapoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers[1][2][3].

IC50& Target[1][2][3]

αvβ3

4 nM (IC50, αvβ3-Vitronectin interaction[2])

αvβ5

79 nM (IC50, αvβ5-Vitronectin interaction[2])

αvβ3

0.61 nM (IC50,[1])

αvβ5

8.4 nM (IC50,[1])

α5β1

14.9 nM (IC50,[1])

STAT3

 

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[2].
Cilengitide inhibits integrin-mediated binding to Vitronectin with IC50s of 0.4 and 0.4 μM in cell adhesion studies assessing the human melanoma M21 or UCLA-P3 human lung carcinoma cell lines[2].
Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC50of 2 μM[2].
Cilengitide (0-1 mg/mL; 24-72 h) inhibits cell viability of melanoma cells in vitro and (5 μg/mL; 12 h) induces B16 and A375 cells apoptosis[3].
Cilengitide (5 μg/mL, 10 μg/mL; 2 weeks) inhibits colony formation of B16 and A375 cells[3].
Cilengitide (0-20 μg/mL; 12 h) inhibits STAT3 phosphorylation to decrease the expression of PD-L1[3].

Western Blot Analysis[3]

Cell Line:B16 and A375 cells
Concentration:0, 5, 10, and 20 μg/mL
Incubation Time:12 hours
Result:Suppressed PD-L1 expression and STAT3 phosphorylation at concentrations greater than 5 μg/mL.

Apoptosis Analysis[3]

Cell Line:B16 and A375 cells
Concentration:5 μg/mL
Incubation Time:12 hours
Result:Resulted apoptosis rates in B16 and A375 cells of 15.27% and 14.89%, respectively.
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[2].
Cilengitide (50 mg/kg; i.p.; daily) enhances the function of CD8+ T cells and promotes anti-PD1 efficacy with Anti-PD1 monoclonal antibody in B16 murine melanoma model[3].

Animal Model:Nude mice bearing M21-L melanoma tumors[2]
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.
Animal Model:Female C57BL/6 mice (6-8 weeks old) with B16 cells s.c.[3]
Dosage:50 mg/kg; with or without 10 mg/kg Anti-PD1 monoclonal antibody or isotype control i.p. every 3 days;
Administration:Intraperitoneal injection; daily
Result:Downregulated the expression of PD-L1 via STAT3 pathway and decreased the expression of PD-L1.
Clinical Trial
分子量

588.66

性状

Solid

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°C3 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.6988 mL8.4939 mL16.9877 mL
5 mM0.3398 mL1.6988 mL3.3975 mL
10 mM0.1699 mL0.8494 mL1.6988 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℃, 6 months; -20℃, 1 month。-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: 100 mg/mL (169.88 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。