Cilengitide trifluoroacetate

別名：EMD 121974, NSC 707544

製品コード：S7077 純度：99.50%

Cilengitide (EMD 121974, NSC 707544) is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

CAS No. 199807-35-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 55500	国内在庫あり
5mg	JPY 40500	国内在庫あり
50mg	JPY 148500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（66）

製品安全説明書

現在のバッチを見る：純度： 99.50%

99.50

Cilengitide trifluoroacetate関連製品

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シグナル伝達経路

Integrinシグナル伝達経路

Integrin阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

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

In Vitro
In vitro	Cilengitide is a cyclized pentapeptide peptidomimetic designed to compete for the arginine-glycine-aspartic acid (RGD) peptide sequence that regulates integrin-ligand binding. Cilengitide selectively and potently blocks the ligation of theαvβ3 andαvβ5 integrins to provisional matrix proteins such as vitronectin, fibronectin, fibrinogen, von Willebrand factor, osteopontin, and others. ^[1] Cilegitide inhibits angiogenesis in vitro. 10 μM Cilengitide completely inhibits attachment of BAE, BME and HUVE cells on vitronectin and fibronectin. Cilengitide inhibits in vitro angiogenesis of BAE cells on three-dimensional collagen and ﬁbrin gels pretreated with FGF-2(or VEGF-A) with IC50 of 15 μM and 8 μM, 4 μM and 3 μM, respectively. ^[2] Cilengitide blocks proliferation and induces apoptosis of endothelial cells as well as differentiation of human endothelial precursor cells (EPCs). 50 μg/mL Cilengitide completely inhibits the proliferation of human microvascular endothelial cell line HMEC-1 and leads to apoptosis in ~30% cells. ^[3] 1.0 μM Cilengitide treating for 9 days inhibits the proliferation of EPCs by nearly 40%. 1 μM Cilengitide inhibits the differentiation of EPCs by more than 80% at 14 days. ^[4] Cilengitide inhibits adhesion and induces apoptosis of tumor cells. 25 μg/mL Cilengitide causes detachment of DAOY cells (medulloblastoma) and U87MG cells (glioblastoma) from vitronectin and tenascin by more than 60%. 25 μg/mL Cilengitide induces a nearly 50% apoptosis rate of these cells. ^[5]
Kinase Assay	Integrin-binding competition assay
Kinase Assay	Recombinant soluble integrins are immobilized, and peptides, which are serially diluted in Tris-buffered saline (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), are added in parallel with biotinylated vitronectin (to 1μg/mL). After a 3-h incubation at 37℃ and washing with Tris–buffered saline, bound ligand is detected by incubation with an antibiotin alkaline phosphatase-conjugated antibody (BioRad) followed by development with p-nitrophenyl phosphatase substrate. The reaction is stopped by the addition of NaOH and the color intensity read at 405 nm.
細胞実験	細胞株	Human microvascular endothelial cell line HMEC-1
	濃度	1-50 μg/mL
	反応時間	3 days
	実験の流れ	HMEC-1 (1×10⁴ per well) are seeded on uncoated 48 well plates and incubated in medium containing 4% FCS with Cilengitide. After incubation for 72 hours at 37℃, cells are trypsinized and counted.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pFAK / p-AKT GLI1		19114005
	Immunofluorescence	VE-cadherin / β3 integrin		19212436
	Growth inhibition assay	Cell number		24153102

In Vivo
In Vivo	Cilengitide is activity against tumor growth and angiogenesis as single-agent. 100 μg Cilengitide induces a significant decrease in the number of CD 31+ vessels seen in tumors (2/high-power field) compared with control tumors (56/high-power field). 100 μg Cilengitide increases cellular apoptosis in the brain tumors of animals (2.2% apoptotic cells/high-power field) compared with those receiving the inactive peptide (1.7% cells/high-power field). Cilengitide treatment results in prolonged survival of the mice bearing melanoma xenografts M21 compared with control treatment group. (36.5 vs 17.3 days). ^[5] Cilengitide can augment the therapeutic benefit associated with cytotoxic agents including chemotherapy and radiation therapy in tumor models. Cilengitide (250 mg/dose) alone does not alter tumor growth of breast cancer xenografts when compared with untreated mice, but combined modality RIT (CMRIT) using RIT and six doses of Cilengitide (250 mg/dose) increases efficacy of treatment, with the cure rate for mice that receives only RIT increasing from 15 to 53%. CMRIT significantly increases apoptosis of tumor and endothelial cells 5 days, and decreases tumor proliferation. ^[6]
動物実験	動物モデル	Human glioblastoma xenografts U87 MG
	投与量	100μg
	投与経路	Daily i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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
[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

参考

+ 展開

化学情報

分子量	702.68	化学式	C₂₉H₄₁F₃N₈O₉
CAS No.	199807-35-7	SDF	Download Cilengitide trifluoroacetate SDFをダウンロードする
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
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (142.31 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 6.25 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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よくある質問（FAQ）

質問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.

質問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):