|2-((2S,5R,8S,11S)-5-苄基-11-(3-胍基丙基)-8-异丙基-7-甲基-3,6,9,12,15-五氧代-1,4,7,10,13-五氮杂环十五烷-2-基)乙酸三氟乙酸盐|CsnPharm

CAS No.: 199807-35-7

Cilengitide TFA/西仑吉肽三氟醋酸盐 Catalog No. CSN19182

Synonyms: EMD 121974 TFA;EMD 121974 Trifluoroacetate;EMD-85189

Cilengitide Trifluoroacetate is a cyclic RGD pentapeptide antagonist of integrins αvβ3, αvβ5 and α5β1.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Integrin αvβ3

IC50:4.1nM Integrin αvβ5

IC50:79nM
描述Integrins are heterodimeric transmembrane receptors involved in a wide range of cancer cell activities. Cilengitide Trifluoroacetate is the trifluoroacetate form of Cilengitide. Cilengitide is a selective and potent inhibitor of αv integrins that blocks the ligation of αvβ3 and αvβ5 integrins to provisional matrix proteins. The IC50 values of cilengitide against αvβ3 and αvβ5 are 4.1 nM and 79 nM, respectively. In primary human brain capillary endothelial cells (BCECs), incubation with 1 μg/mL cilengitide for 1h decreased cell adhesion to vitronectin. When cilengitide was added 1h after the attachment of BCECs to vitronectin, the detachment occurred in a dose-dependent manner, and the significant detachment was observed at the concentration of 10 μg/mL or higher. In αv-integrin-expressing tumor cell lines U87MG and DAOY, the exposure of 25 μg/ml cilengitide for 24h led to a significant increase in apoptosis compared to cells treated with control peptide. In a mouse xenograft model established by injecting αv-positive melanoma cells into the forebrain, Cilengitide treatment resulted in an average survival of 36.5 days compared to 17.3 days in the control peptide-treated animals.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CAL27	6.25–200 µM	Growth Inhibition Assay	72 h	results moderate, dose-dependent growth inhibition	24557056
CAL27	25 µM	Apoptosis Assay	48 h	induces apoptosis	24557056
FaDu	6.25–200 µM	Growth Inhibition Assay	72 h	results moderate, dose-dependent growth inhibition	24557056

更多
动物研究
剂量
Mice: 20 mg/kg^[3] (i.v.)

给药途径
i.v.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.v.)
给药途径	i.v.

[1] Reardon DA, Cheresh D. Cilengitide: a prototypic integrin inhibitor for the treatment of glioblastoma and other malignancies. Genes Cancer. 2011 Dec;2(12):1159-65.
[2] Nisato RE, Tille JC, et al. alphav beta 3 and alphav beta 5 integrin antagonists inhibit angiogenesis in vitro. Angiogenesis. 2003;6(2):105-19.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4231 mL
- 7.1156 mL
- 14.2312 mL
- 5 mM
- 0.2846 mL
- 1.4231 mL
- 2.8462 mL
- 10 mM
- 0.1423 mL
- 0.7116 mL
- 1.4231 mL

技术信息

CAS号

199807-35-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H41F3N8O9

运输

蓝冰

分子量

702.68

别名

EMD 121974 TFA;EMD 121974 Trifluoroacetate;EMD-85189;EMD-121974;NSC-707544;D03497;Cyclo(L-arginylglycyl-L-aspartyl-D-phenylalanyl-N-methyl-L-valyl)

溶解度

DMSO	280.0 mg/mL (398.5 mM) warming
Water	100.0 mg/mL (142.3 mM) warming

动物实验配方

0.5% CMC-Na

40 mg/mL

clear

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

CAL27	6.25–200 µM	Growth Inhibition Assay	72 h	results moderate, dose-dependent growth inhibition	24557056
CAL27	25 µM	Apoptosis Assay	48 h	induces apoptosis	24557056
FaDu	6.25–200 µM	Growth Inhibition Assay	72 h	results moderate, dose-dependent growth inhibition	24557056
FaDu	25 µM	Apoptosis Assay	48 h	induces apoptosis	24557056
G28	1/5/50 μg/ml	Proliferation Assay	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
G28	1/5/50 μg/ml	Apoptosis Assay	24 h	induces apoptosis	19114005
G28	50 μg/ml	Function Assay	30/60/120 min	inhibits phosphorylation of FAK, Src and Akt	19114005
G44	1/5/50 μg/ml	Proliferation Assay	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
G44	1/5/50 μg/ml	Apoptosis Assay	24 h	induces apoptosis	19114005
H28	1 nM-200 μM	Cell Viability Assay	72 h	decreases cell viability in a dose dependent manner	24595274
HaCaT	10 μm	Function Assay	48 h	reduces TGF-β2 mRNA expression	26500056
HMEC-1	1/5/50 μg/ml	Function Assay	24 h	induces a dose dependent detachment	19114005
HMEC-1	1/5/50 μg/ml	Proliferation Assay	24/48/72 h	inhibits proliferation in a dose dependent manner	19114005
HMEC-1	1/5/50 μg/ml	Apoptosis Assay	24 h	induces apoptosis	19114005
HMEC-1	20/40/60 μg/ml	Function Assay	-	inhibits FAK and Src	19114005
LN-18	0.1/1/10 μM	Function Assay	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
LN-308	1/10/100 μm	Function Assay	24 h	reduces DRE reporter activity in a concentration-dependent manner	26500056
LN-308	10 μm	Function Assay	24 h	reduces AhR protein levels and DRE reporter activity	26500056
LN-308	0.1/1/10 μM	Function Assay	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
LNT-229	0.1/1/10 μM	Function Assay	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
MCF-7	0-20 μM	Growth Inhibition Assay	96 h	inhibits cell growth in a dose dependent manner	24153102
MCF-7	0-20 μM	Apoptosis Assay	48 h	induces apoptosis	24153102
MM05	1 nM-200 μM	Cell Viability Assay	72 h	decreases cell viability in a dose dependent manner	24595274
MSTO-211H	1 nM-200 μM	Cell Viability Assay	72 h	decreases cell viability in a dose dependent manner	24595274
REN	1 nM-200 μM	Cell Viability Assay	72 h	decreases cell viability in a dose dependent manner	24595274
S-24	1/10 μm	Function Assay	24 h	reduces DRE reporter activity	26500056
SCC25	6.25–200 µM	Growth Inhibition Assay	72 h	results moderate, dose-dependent growth inhibition	24557056
SCC25	25 µM	Apoptosis Assay	48 h	induces apoptosis	24557056
T-47D	0-20 μM	Growth Inhibition Assay	96 h	inhibits cell growth in a dose dependent manner	24153102
T-47D	0-20 μM	Apoptosis Assay	48 h	induces apoptosis	24153102
T98G	0.1/1/10 μM	Function Assay	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
U251	0-25 μg/mL	Growth Inhibition Assay	0-48 h	inhibits cell growth in dose and time dependent manner	21788343
U251	25 μg/mL	Apoptosis Assay	24/48 h	induces apoptosis at 48 h significantly	21788343
U251	0-25 μg/mL	Function Assay	12 h	induces autophagy dose dependently	21788343
U251MG	0-25 μM	Growth Inhibition Assay	24/48 h	inhibits cell growth in dose and time dependent manner	23354807
U251MG	1 µM	Apoptosis Assay	48 h	induces apoptosis	23354807
U87	0-25 μg/mL	Growth Inhibition Assay	0-48 h	inhibits cell growth in dose and time dependent manner	21788343
U87	25 μg/mL	Apoptosis Assay	24/48 h	induces apoptosis at 48 h significantly	21788343
U87	0-25 μg/mL	Function Assay	12 h	induces autophagy dose dependently	21788343
U87MG	0-25 μM	Growth Inhibition Assay	24/48 h	inhibits cell growth in dose and time dependent manner	23354807
U87MG	1 µM	Apoptosis Assay	48 h	induces apoptosis	23354807
U87MG	0.1/1/10 μM	Function Assay	24 h	impairs the adhesion of cells to vitronectin in a dose dependent manner	19221171
ZH-161	1/10 μm	Function Assay	24 h	reduces DRE reporter activity	26500056

靶点	Description	IC50
Integrin αvβ3		IC50:4.1nM
Integrin αvβ5		IC50:79nM

Cilengitide TFA/西仑吉肽 三氟醋酸盐 Catalog No. CSN19182

靶点选择性

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确认信息

Cilengitide TFA/西仑吉肽三氟醋酸盐 Catalog No. CSN19182