Cyclo(-RGDfK) TFA

製品コードS7834 バッチS783404

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₉H₄₂F₃N₉O₉

分子量

717.69

CAS No.

500577-51-5

Solubility (25°C)*

体外

DMSO

100 mg/mL (139.33 mM)

Water

100 mg/mL (139.33 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (6.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.830mg/ml (1.16mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Cyclo(-RGDfK) TFA is the salt product of Cyclo(-RGDfK) and trifluoroacetic acid (TFA). The addition of TFA enhances stability and biocompatibility. Cyclo(-RGDfK) TFA effectively targets tumor microvessels and cancer cells by specifically binding to the cell surface Integrin αvβ3.
in vitro	The constant of affinity (K_D) of Cyclo (-RGDfK-) for purified integrin is 41.70 nM.^[2] This compound is reacting with HEK293(β3) cells moderately.^[3] This compound modified micelles shows strong affinity to T-24 cells and strong inhibitory effect on the proliferation of T-24 cells.^[4]
in vivo	In athymic mice bearing α(v)β(3)-integrin-positive C6 gliomas, Cyclo (-RGDfK-) TFA modification induces less tumor progression, less tumor metabolic activity, fewer intratumoral vessels.^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Isolated Integrin Binding Assays.
キナーゼアッセイ	Purified integrin (1 μg/mL; 4℃) is used to coat 96-well microtitre plates, which are then blocked with bovine serum albumin (BSA) (3% in 1 mM CaCl_{2, 1 mM MgCl_{2,10 pM MnCl2, 100 mM NaC1,50 mM trishydroxymethyl-aminomethane; pH 7.4), and incubated (3 h at 30 ℃) with biotinylated ligands (1 pg/mL in binding buffer: 0.1% BSA, 1 mM CaCl2,1 mM MgCl2, 10 μM MnCl2, 100 mM NaCl, 50 mM trishydroxymethyl-aminomethane; pH 7.4) in the presence or absence of serially diluted peptides. After washing (3×5 min with binding buffer), bound biotinylated ligand is detected with alkaline-phosphatase conjugated goat antibiotin antibodies (1 μg/mL; 1 h, 37℃), using p-nitrophenyl phosphate as chromogen. This compound binding in the absence of competitor is defined as 100% signal; binding to blocked wells in the absence of integrin is defined as 0%. Concentrations of this chemical required for 50% inhibition of signal (IC50 values) are estimated graphically.}}
細胞アッセイ	細胞株	T-24 cells
	濃度
	反応時間	72 h
	実験の流れ	T-24 cells are seeded in 96-well plate at a density of 5000 cells per well and incubated for 24 h to allow the cells to grow to 80% conﬂuence. This compound is added and incubated with cells for 72 h. Then 200 μL fresh F-12 without fetal bovine serum but containing 10 μL MTS solution is added.

参考

http://www.sciencedirect.com/science/article/pii/S0040403900010601
https://pubmed.ncbi.nlm.nih.gov/19259068/
https://pubmed.ncbi.nlm.nih.gov/17565663/

https://pubmed.ncbi.nlm.nih.gov/23388072/
https://pubmed.ncbi.nlm.nih.gov/24730235/
https://pubmed.ncbi.nlm.nih.gov/10452325/

+ 展开

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Radioiodinated Bicyclic RGD Peptide Derivatives for Enhanced Tumor Accumulation [ Pharmaceuticals (Basel), 2025, 18(4)549]	PubMed: 40283983
Dentin matrix protein-1 promoted osteogenic differentiation of valvular interstitial cells via MAPK signal pathway during aortic valve calcification [ In Vitro Cell Dev Biol Anim, 2025, 10.1007/s11626-025-01101-7]	PubMed: 41082151
Acute contact with profibrotic macrophages mechanically activates fibroblasts via αvβ3 integrin-mediated engagement of Piezo1 [ Sci Adv, 2024, 10(43):eadp4726]	PubMed: 39441936
Tenascin-C in the early lung cancer tumor microenvironment promotes progression through integrin αvβ1 and FAK [ bioRxiv, 2024, 2024.09.17.613509]	PubMed: 39345541
SPARC Aggravates Blood-Brain Barrier Disruption via Integrin [ Oxidative Medicine and Cellular Longevity, 2021, 10.1155/2021/9739977]	PubMed: None
SPARC Aggravates Blood-Brain Barrier Disruption via Integrin αVβ3/MAPKs/MMP-9 Signaling Pathway after Subarachnoid Hemorrhage [ Oxid Med Cell Longev, 2021, 2021:9739977]	PubMed: 34804372
Integrin αv and Vitronectin Prime Macrophage-Related Inflammation and Contribute the Development of Dry Eye Disease [ Int J Mol Sci, 2021, 22(16)8410]	PubMed: 34445121
MOB2 suppresses GBM cell migration and invasion via regulation of FAK/Akt and cAMP/PKA signaling. [ Cell Death Dis, 2020, 14;11(4):230]	PubMed: 32286266
MiR-30 family prevents uPAR-ITGB3 signaling activation through calcineurin-NFATC pathway to protect podocytes [ Cell Death Dis, 2019, 10(6):401]	PubMed: 31127093
CCN1 interlinks integrin and hippo pathway to autoregulate tip cell activity. [ Elife, 2019, 8]	PubMed: 31429823

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。