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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C29H42F3N9O9 |
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分子量 | 717.69 | CAS No. | 500577-51-5 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (139.33 mM) | |
Water | 84 mg/mL (117.04 mM) | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor. |
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in vitro | The constant of affinity (KD) of Cyclo (-RGDfK-) for purified integrin is 41.70 nM.[2] Cyclo (-RGDfK) is reacting with HEK293(β3) cells moderately.[3] Cyclo(-RGDfK-) 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-) modification induces less tumor progression, less tumor metabolic activity, fewer intratumoral vessels.[5] |
キナーゼアッセイ | Isolated Integrin Binding Assays. | |
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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 CaCl2, 1 mM MgCl2,10 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. Cyclo (-RGDfK) 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 Cyclo (-RGDfK) 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. Drugs are 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. |
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 |
Tension enhances cell proliferation and collagen synthesis by upregulating expressions of integrin αvβ3 in human keloid-derived mesenchymal stem cells [Song H Life Sci, 2019, 219:272-282] | PubMed: 30597173 |
Acquired Resistance to EGFR TKIs Mediated by TGFβ1/Integrin β3 Signaling in EGFR-Mutant Lung Cancer [ Mol Cancer Ther, 2019, 18(12):2357-2367] | PubMed: 31501278 |
Acquired resistance to EGFR TKIs mediated by TGF-beta1/integrin beta3 signaling in EGFR-mutant lung cancer. [ Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0181] | PubMed: 31501278 |
Spontaneous Extracellular Matrix Accumulation in a Human in vitro Model of Renal Fibrosis Is Mediated by αV Integrins [ Nephron, 2019, 10.1159/000499506] | PubMed: 31048591 |
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。