Cilengitide 西仑吉肽; EMD 121974|cas:188968-51-6|西域试剂

Cilengitide 西仑吉肽; EMD 121974,99.70%

产品编号：Bellancom-16141| CAS NO：188968-51-6| 分子式：C₂₇H₄₀N₈O₇| 分子量：588.66

Cilengitide是有效，选择性的αvβ3 和αvβ5受体整合素抑制剂，IC50分别为4和79 nM。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16141	￥1220.00	杭州北京（现货）
Bellancom-16141	￥1730.00	杭州北京（现货）
Bellancom-16141	￥5500.00	杭州北京（现货）
Bellancom-16141	￥8500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Cilengitide 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 (α_νβ₃)，8.4 nM (α_νβ₅) 和 14.9 nM (α₅β₁)。Cilengitide 抑制 α_νβ₃ 和 α_νβ₅ 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 potent integrins antagonist with IC₅₀s of 0.61 nM (α_νβ₃), 8.4 nM (α_νβ₅) and 14.9 nM (α₅β₁), respectively. Cilengitide inhibits the binding of α_νβ₃ and α_νβ₅ to Vitronectin with IC₅₀s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.

体外研究

Cilengitide is a cyclized RGD (Arg-Gly-Asp motif)-containing pentapeptide. Cilengitide blocks integrin ανβ3- and ανβ5-mediated endothelial cell attachment and migration.
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.
Cilengitide inhibits the attachment of human umbilical vein endothelial cells to Vitronectin with an IC₅₀ of 2 μM.
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.
Cilengitide (5 μg/mL, 10 μg/mL; 2 weeks) inhibits colony formation of B16 and A375 cells.
Cilengitide (0-20 μg/mL; 12 h) inhibits STAT3 phosphorylation to decrease the expression of PD-L1.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing M21-L melanoma tumors
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.
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing M21-L melanoma tumors
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.
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing M21-L melanoma tumors
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.
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.

性状

Solid

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。

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西域网站选购。

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

参考文献

. Kapp TG, et al. A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins. Sci Rep. 2017 Jan 11;7:39805. [Content Brief]

. 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. [Content Brief]

. Pan X, et al. Cilengitide, an αvβ3-integrin inhibitor, enhances the efficacy of anti-programmed cell death-1 therapy in a murine melanoma model. Bioengineered. 2022 Feb;13(2):4557-4572. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Cilengitide
CAS号：	188968-51-6
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Cilengitide
别名：	EMD 121974, NSC 707544
分子式：	C27H40N8O7
分子量：	588.66

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	-20°C, dry, sealed

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

199807-35-7

188968-51-6

文献：US7115261 B1, ; Page/Page column 20 ;

上游产品 1
199807-35-7
下游产品 1
188969-00-8

[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.

[3]. Ten Hagen TL, et al. The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model. Int J Cancer. 2012 Nov 13. [Epub ahead of print]

Cilengitide 西仑吉肽; EMD 121974,99.70%

Cilengitide 西仑吉肽; EMD 121974

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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