Cilengitide?trifluoroacetate

別名: EMD 121974, NSC 707544 中文名稱：三氟醋酸鹽西侖吉肽

目錄號：S7077 Purity: 99.50%

Cilengitide (EMD 121974, NSC 707544)是一種有效的integrin抑制劑，作用于αvβ3受體和αvβ5受體，無細(xì)胞試驗中IC50分別為4.1 nM和79 nM，比作用于gpIIbIIIa選擇性高10倍左右。Phase 2。

Cilengitide?trifluoroacetate Chemical Structure

CAS: 199807-35-7

規(guī)格	價格	庫存
10mM (1mL in DMSO)	3718.02	現(xiàn)貨
5mg	2212.59	現(xiàn)貨
50mg	8108.38	現(xiàn)貨
1g	32678.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.50%

99.50

Cilengitide?trifluoroacetate相關(guān)產(chǎn)品

相關(guān)靶點	ILK	點擊展開
相關(guān)產(chǎn)品	Cilengitide SB273005 RGD (Arg-Gly-Asp) Peptides ATN-161 Cyclo(RGDyK) Cyclo(-RGDfK) TFA Leukadherin-1 A-205804 OSU-T315	點擊展開
相關(guān)化合物庫	激酶抑制劑庫血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫細(xì)胞骨架信號通路化合物庫抗心血管疾病化合物庫	點擊展開

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻(xiàn)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
點擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

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

體外研究(In Vitro)
體外研究活性	Cilengitide是一種環(huán)化五勝肽類肽，爭奪精氨酸-甘氨酸-天冬氨酸（RGD）肽序列。調(diào)節(jié)整合素-配體結(jié)合。Cilengitide選擇性且有效抑制αvβ3和αvβ5整合素與基質(zhì)蛋白結(jié)合，如Vitronectin, Fibronectin, Fibrinogen, von Willebrand Factor, Osteopontin, 及其他。^[1]10 μM Cilengitide完全抑制BAE，BME和HUVE細(xì)胞與Vitronectin 和 Fibronectin附著。Cilengitide在體外作用于三維膠原蛋白和血纖維蛋白凝膠使用FGF-2(或 VEGF-A)預(yù)處理的BAE細(xì)胞，抑制血管生成，IC50分別為15 μM 和8 μM, 4 μM 和 3 μM。^[2]Cilengitide 抑制細(xì)胞增殖，誘導(dǎo)內(nèi)皮細(xì)胞凋亡，且誘導(dǎo)人體內(nèi)皮前體細(xì)胞分化。50 μg/mL Cilengitide完全抑制人體微血管內(nèi)皮細(xì)胞系HMEC-1增殖，導(dǎo)致?30%細(xì)胞發(fā)生細(xì)胞凋亡。^[3]1 μM Cilengitide處理9天，抑制近40%EPCs增殖。1 μM Cilengitide處理14天，抑制80%以上EPCs 分化。^[4]Cilengitide抑制粘附，誘導(dǎo)腫瘤細(xì)胞凋亡。25 μg/mL Cilengitide使60%以上的DAOY細(xì)胞(髓母細(xì)胞瘤)和U87MG細(xì)胞(膠質(zhì)母細(xì)胞瘤) 與Vitronectin 和 Tenascin分離。25 μg/mL Cilengitide誘導(dǎo)細(xì)胞凋亡率將近50% 。^[5]
激酶實驗	整合素競爭結(jié)合實驗
激酶實驗	固定化重組可溶性的整合素，同時加入在Tris 緩沖生理鹽水(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)中連續(xù)稀釋的肽，及生物素化的Vitronectin（1μg/mL）。在37°C下溫育3小時后，使用Tris 緩沖生理鹽水洗滌，通過與抗生物素的堿性磷酸酶聯(lián)合的抗體溫育，再經(jīng)對硝基苯基磷酸酶底物顯影，測定結(jié)合的配體。加入NaOH終止反應(yīng)，在405 nm處讀取彩色信號強度。
細(xì)胞實驗	細(xì)胞系	人體微血管內(nèi)皮細(xì)胞系HMEC-1
	濃度	1-50 μg/mL
	孵育時間	3 天
	方法	HMEC-1 按每孔1×10⁴個接種在未包被的48孔板中，在含4% FCS 及 Cilengitide的培養(yǎng)基中溫育。在37°C下溫育72小時, 用胰蛋白酶處理細(xì)胞并計數(shù)。
實驗圖片	檢測方法	檢測指標(biāo)	實驗圖片	PMID
	Western blot	GLI1 pFAK / p-AKT		31366904
	Immunofluorescence	VE-cadherin / β3 integrin		19212436
	Growth inhibition assay	Cell number		24153102

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Cilengitide單獨處理，有效對抗腫瘤生長和血管生成。100 μg Cilengitide處理腫瘤，與對照組相比，顯著降低CD31⁺血管數(shù)。100 μg Cilengitide處理動物大腦中的腫瘤，與接收無效肽處理的相比，促進(jìn)細(xì)胞凋亡。Cilengitide 處理攜帶黑色素移植瘤M21的小鼠，對照組相比，延長小鼠壽命，分別為36.5 天vs 17.3天。^[5]Cilengitide 可以增加細(xì)胞毒性藥物相關(guān)聯(lián)的治療的益處，包括對腫瘤模型的化療和放射治療。Cilengitide (250 mg/dose)單獨處理小鼠，與未經(jīng)處理的小鼠相比，沒有改變?nèi)橄侔┮浦擦龅哪[瘤生長，但與RIT（CMRIT）聯(lián)合治療，使用RIT和六種劑量的Cilengitide (250 mg/dose)增加治療的療效，小鼠的治愈率從只用RIT處理的 15%提高到53％。CMRIT處理內(nèi)皮細(xì)胞5天，顯著促進(jìn)腫瘤細(xì)胞凋亡，且降低腫瘤細(xì)胞增殖。^[6]
動物實驗	Animal Models	攜帶人體膠質(zhì)母細(xì)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
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01517776	Terminated	Gliomas	Martin-Luther-Universit?t 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

參考文獻(xiàn)
[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. + 展開

參考文獻(xiàn)

[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.

+ 展開

化學(xué)信息&溶解度

分子量	702.68	分子式	C₂₉H₄₁F₃N₈O₉
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (142.31 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 6.25 mg/mL (8.89 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (142.31 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 25 mg/mL (35.57 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (142.31 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 6.25 mg/mL (8.89 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊

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常見問題及建議解決方法

問題 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.

問題 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):

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Cilengitide?trifluoroacetate

產(chǎn)品質(zhì)控

Cilengitide?trifluoroacetate相關(guān)產(chǎn)品

相關(guān)信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

技術(shù)支持

常見問題及建議解決方法