Cilengitide trifluoroacetate

别名: EMD 121974, NSC 707544 中文名称：三氟醋酸盐西仑吉肽

目录号：S7077 Purity: 99.50%

Cilengitide (EMD 121974, NSC 707544)是一种有效的integrin抑制剂，作用于αvβ3受体和αvβ5受体，无细胞试验中IC50分别为4.1 nM和79 nM，比作用于gpIIbIIIa选择性高10倍左右。Phase 2。

Cilengitide trifluoroacetate Chemical Structure

CAS: 199807-35-7

规格	价格	库存
10mM (1mL in DMSO)	RMB 3718.02	现货
5mg	RMB 2212.59	现货
50mg	RMB 8108.38	现货
1g	RMB 32678.1	现货
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客户使用Selleck的Cilengitide trifluoroacetate发表文献66篇

产品质控

批次：纯度： 99.50%

99.50

Cilengitide trifluoroacetate相关产品

相关靶点	ILK	点击展开
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Integrin抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
MCF-7	Apoptosis Assay	0-20 μM	48 h	induces apoptosis	24153102
U87MG	Growth Inhibition Assay	0-25 μM	24/48 h	inhibits cell growth in dose and time dependent manner	23354807
U251MG	Growth Inhibition Assay	0-25 μM	24/48 h	inhibits cell growth in dose and time dependent manner	23354807
U87MG	Apoptosis Assay	1 µM	48 h	induces apoptosis	23354807
U251MG	Apoptosis Assay	1 µM	48 h	induces apoptosis	23354807
U251	Growth Inhibition Assay	0-25 μg/mL	0-48 h	inhibits cell growth in dose and time dependent manner	21788343
U87	Growth Inhibition Assay	0-25 μg/mL	0-48 h	inhibits cell growth in dose and time dependent manner	21788343
U251	Apoptosis Assay	25 μg/mL	24/48 h	induces apoptosis at 48 h significantly	21788343
U87	Apoptosis Assay	25 μg/mL	24/48 h	induces apoptosis at 48 h significantly	21788343
U251	Function Assay	0-25 μg/mL	12 h	induces autophagy dose dependently	21788343
U87	Function Assay	0-25 μg/mL	12 h	induces autophagy dose dependently	21788343
U87MG	Function Assay	0.1/1/10 μM	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
LN-308	Function Assay	0.1/1/10 μM	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
LN-18	Function Assay	0.1/1/10 μM	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
T98G	Function Assay	0.1/1/10 μM	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
LNT-229	Function Assay	0.1/1/10 μM	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
HMEC-1	Function Assay	1/5/50 μg/ml	24 h	induces a dose dependent detachment	19114005
HMEC-1	Proliferation Assay	1/5/50 μg/ml	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
HMEC-1	Apoptosis Assay	1/5/50 μg/ml	24 h	induces apoptosis	19114005
G28	Proliferation Assay	1/5/50 μg/ml	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
G44	Proliferation Assay	1/5/50 μg/ml	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
G28	Apoptosis Assay	1/5/50 μg/ml	24 h	induces apoptosis	19114005
G44	Apoptosis Assay	1/5/50 μg/ml	24 h	induces apoptosis	19114005
G28	Function Assay	50 μg/ml	30/60/120 min	inhibits phosphorylation of FAK, Src and Akt	19114005
T-47D	Apoptosis Assay	0-20 μM	48 h	induces apoptosis	24153102
MCF-7	Growth Inhibition Assay	0-20 μM	96 h	inhibits cell growth in a dose dependent manner	24153102
T-47D	Growth Inhibition Assay	0-20 μM	96 h	inhibits cell growth in a dose dependent manner	24153102
FaDu	Apoptosis Assay	25 µM	48 h	induces apoptosis	24557056
CAL27	Apoptosis Assay	25 µM	48 h	induces apoptosis	24557056
SCC25	Apoptosis Assay	25 µM	48 h	induces apoptosis	24557056
FaDu	Growth Inhibition Assay	6.25–200 µM	72 h	results moderate, dose-dependent growth inhibition	24557056
CAL27	Growth Inhibition Assay	6.25–200 µM	72 h	results moderate, dose-dependent growth inhibition	24557056
SCC25	Growth Inhibition Assay	6.25–200 µM	72 h	results moderate, dose-dependent growth inhibition	24557056
H28	Cell Viability Assay	1 nM-200 μM	72 h	decreases cell viability in a dose dependent manner	24595274
MM05	Cell Viability Assay	1 nM-200 μM	72 h	decreases cell viability in a dose dependent manner	24595274
MSTO-211H	Cell Viability Assay	1 nM-200 μM	72 h	decreases cell viability in a dose dependent manner	24595274
REN	Cell Viability Assay	1 nM-200 μM	72 h	decreases cell viability in a dose dependent manner	24595274
LN-308	Function Assay	10 μm	24 h	reduces AhR protein levels and DRE reporter activity	26500056
HaCaT	Function Assay	10 μm	48 h	reduces TGF-β2 mRNA expression	26500056
S-24	Function Assay	1/10 μm	24 h	reduces DRE reporter activity	26500056
ZH-161	Function Assay	1/10 μm	24 h	reduces DRE reporter activity	26500056
LN-308	Function Assay	1/10/100 μm	24 h	reduces DRE reporter activity in a concentration-dependent manner	26500056
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs by Western blot method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 by Western blot method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by Western blot method	29775303
U87MG	Function assay	100 nM	8 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by RT-PCR method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs by RT-PCR method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 by RT-PCR method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 by RT-PCR method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by RT-PCR method	29775303
U87MG	Function assay	100 nM	24 hrs	Inhibition of alphaVbeta3 integrin in human U87MG cells assessed as increase in p21 mRNA expression at 100 nM after 24 hrs by RT-PCR method	29775303
U87MG	Antiproliferative assay	100 nM	72 hrs	Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of MDM2 inhibitor nutlin-3 by MTS assay	29775303
U87MG	Antiproliferative assay	100 nM	72 hrs	Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by MTS assay	29775303
U87MG	Cell cycle assay	100 nM	24 hrs	Cell cycle arrest in human U87MG cells assessed as accumulation at G0/G1 phase at 100 nM after 24 hrs	29775303
U87MG	Anti-invasive assay	10 uM	24 hrs	Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs by transwell assay	29775303
U87MG	Anti-invasive assay	10 uM	24 hrs	Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs in presence of MDM2 inhibitor nutlin-3 and MDM4 inhibitor SJ-1722550 by transwell assay	29775303
HMEC-1	Function Assay	20/40/60 μg/ml		inhibits FAK and Src	19114005
M21	Function assay		1 hr	Binding affinity to integrin alphav/beta3 heterodimer in human M21 cells assessed as inhibition of integrin-mediated human M21 cell adhesion to vitronectin after 1 hr in presence of MnCl2, IC50 = 0.0004 μM.	26753814
HEK293T	Function assay		2 hrs	Binding affinity to soluble truncated human recombinant Fc-tagged alphaVbeta3 and integrins were expressed in HEK293T cells after 2 hrs by competition ELISA-like assay, IC50 = 0.00051 μM.	24095096
HT-29	Function assay		2 hrs	Antagonist activity at integrin alphaVbeta5 (unknown origin) expressed in HT-29 cells assessed as reduction in cell adhesion to vitronectin after 2 hrs by MTT assay, IC50 = 0.12 μM.	28351594
HEK293	Function assay		2 hrs	Antagonist activity at integrin alphaVbeta3 (unknown origin) expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay, IC50 = 0.22 μM.	28351594
SKOV3	Function assay		2 hrs	Antagonist activity at integrin alphaVbeta3alphaVbeta5 (unknown origin) expressed in SKOV3 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay, IC50 = 0.37 μM.	28351594
点击查看更多细胞系数据

生物活性

产品描述

靶点

αvβ3 receptor ^[1] (Cell-free assay)	αvβ5 receptor ^[2] (Cell-free assay)
4.1 nM	79 nM

体外研究(In Vitro)
体外研究活性	Cilengitide是一种环化五胜肽类肽，争夺精氨酸-甘氨酸-天冬氨酸（RGD）肽序列。调节整合素-配体结合。Cilengitide选择性且有效抑制αvβ3和αvβ5整合素与基质蛋白结合，如Vitronectin, Fibronectin, Fibrinogen, von Willebrand Factor, Osteopontin, 及其他。^[1]10 μM Cilengitide完全抑制BAE，BME和HUVE细胞与Vitronectin 和 Fibronectin附着。Cilengitide在体外作用于三维胶原蛋白和血纤维蛋白凝胶使用FGF-2(或 VEGF-A)预处理的BAE细胞，抑制血管生成，IC50分别为15 μM 和8 μM, 4 μM 和 3 μM。^[2]Cilengitide 抑制细胞增殖，诱导内皮细胞凋亡，且诱导人体内皮前体细胞分化。50 μg/mL Cilengitide完全抑制人体微血管内皮细胞系HMEC-1增殖，导致〜30%细胞发生细胞凋亡。^[3]1 μM Cilengitide处理9天，抑制近40%EPCs增殖。1 μM Cilengitide处理14天，抑制80%以上EPCs 分化。^[4]Cilengitide抑制粘附，诱导肿瘤细胞凋亡。25 μg/mL Cilengitide使60%以上的DAOY细胞(髓母细胞瘤)和U87MG细胞(胶质母细胞瘤) 与Vitronectin 和 Tenascin分离。25 μg/mL Cilengitide诱导细胞凋亡率将近50% 。^[5]
激酶实验	整合素竞争结合实验
激酶实验	固定化重组可溶性的整合素，同时加入在Tris 缓冲生理盐水(TBS++) (0.1% (w/v) BSA, 150 mM NaCl, 1 mM CaCl₂, 1 mM MgCl₂ 10 μM MnCl₂, 20 mM Tris-HCl; pH 7.4)中连续稀释的肽，及生物素化的Vitronectin（1μg/mL）。在37°C下温育3小时后，使用Tris 缓冲生理盐水洗涤，通过与抗生物素的碱性磷酸酶联合的抗体温育，再经对硝基苯基磷酸酶底物显影，测定结合的配体。加入NaOH终止反应，在405 nm处读取彩色信号强度。
细胞实验	细胞系	人体微血管内皮细胞系HMEC-1
	浓度	1-50 μg/mL
	孵育时间	3 天
	方法	HMEC-1 按每孔1×10⁴个接种在未包被的48孔板中，在含4% FCS 及 Cilengitide的培养基中温育。在37°C下温育72小时, 用胰蛋白酶处理细胞并计数。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	pFAK / p-AKT GLI1		19114005
	Immunofluorescence	VE-cadherin / β3 integrin		19212436
	Growth inhibition assay	Cell number		24153102

体内研究(In Vivo)
体内研究活性	Cilengitide单独处理，有效对抗肿瘤生长和血管生成。100 μg Cilengitide处理肿瘤，与对照组相比，显著降低CD31⁺血管数。100 μg Cilengitide处理动物大脑中的肿瘤，与接收无效肽处理的相比，促进细胞凋亡。Cilengitide 处理携带黑色素移植瘤M21的小鼠，对照组相比，延长小鼠寿命，分别为36.5 天vs 17.3天。^[5]Cilengitide 可以增加细胞毒性药物相关联的治疗的益处，包括对肿瘤模型的化疗和放射治疗。Cilengitide (250 mg/dose)单独处理小鼠，与未经处理的小鼠相比，没有改变乳腺癌移植瘤的肿瘤生长，但与RIT（CMRIT）联合治疗，使用RIT和六种剂量的Cilengitide (250 mg/dose)增加治疗的疗效，小鼠的治愈率从只用RIT处理的 15%提高到53％。CMRIT处理内皮细胞5天，显著促进肿瘤细胞凋亡，且降低肿瘤细胞增殖。^[6]
动物实验	Animal Models	携带人体胶质母细胞瘤移植瘤U87 MG的小鼠
	Dosages	100μg
	Administration	每天腹腔注射

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01517776	Terminated	Gliomas	Martin-Luther-Universität Halle-Wittenberg\|Merck KGaA Darmstadt Germany	January 2012	Phase 2
NCT01118676	Completed	Locally Advanced Non Small Cell Lung Cancer (NSCLC)	Institut Claudius Regaud\|Merck KGaA Darmstadt Germany	March 2010	Phase 1

参考文献
[1] Reardon DA, et al. Genes Cancer, 2011, 2(12):1159-1165. [2] Nisato RE, et al. Angiogenesis, 2003, 6(2), 105-119. [3] Oliveira-Ferrer L, et al. J Exp Clin Cancer Res, 2008, 27:86. [4] Loges S, et al. Biochem Biophys Res Commun, 2007, 357(4), 1016-1020 [5] Taga T, et al. Int J Cancer, 2002, 98(5):690-697. [6] Burke PA, et al. Cancer Res, 2002, 62(15), 4263-4272. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	702.68	分子式	C₂₉H₄₁F₃N₈O₉
CAS号	199807-35-7	SDF	Download Cilengitide trifluoroacetate SDF
Smiles	CC(C)C1C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N.C(=O)(C(F)(F)F)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (142.31 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 6.25 mg/mL

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
The recommend vehicle is 30% propylene glycol, 5% Tween 80, 65% D5W at 30mg/ml, can you let me know if this is a suspension or clear solution?

回答：
S7077 Cilengitide can be dissolved in 30% propylene glycol/5% Tween 80/65% D5W at 10 mg/ml as a clear solution.

问题 2:
Is Cilengitide a TFA salt?

回答：
S7077 Cilengitide is actually a TFA salt, and the ratio between Cilengitide and TFA is 1:1.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):