受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
|
化学式 | C13H10BrN3O4 |
|||
分子量 | 352.14 | CAS No. | 182498-32-4 | |
Solubility (25°C)* | 体外 | DMSO | 70 mg/mL (198.78 mM) | |
Ethanol | 14 mg/mL warmed with 50ºC water bath (39.75 mM) | |||
Water | 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 | SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested. |
---|---|
in vitro | In vitro, SB225002 inhibits GROα-stimulated calcium mobilization, and potently inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha. [1] SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. [2] SB225002 also shows the antitumor activity as a microtubule inhibitor. [3] |
in vivo | In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. [1] In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. [4] In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models. [5] [6] |
キナーゼアッセイ | Radioligand Binding Experiments | |
---|---|---|
Assays are performed in 96-well microtiter plates where the reaction mixture contains 1.0 μg/ml membrane protein in 20 mM Bis-Tris-propane, pH 8.0, with 1.2 mM MgSO4, 0.1 mM EDTA, 25 mM NaCl, and 0.03% CHAPS and SB 225002 (10 mM stock in Me2SO) added at the indicated concentrations, the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8 (2,200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine, 0.5% BSA and washed three times with 25 mM NaCl, 10 mM Tris·HCl, 1 mM MgSO4, 0.5 mM EDTA, 0.03% CHAPS, pH 7.4. The filter is dried, sealed in a sample bag containing 10 ml of Wallac 205 Betaplate liquid scintillation fluid, and counted with a Wallac 1205 Betaplate liquid scintillation counter. | ||
細胞アッセイ | 細胞株 | WHCO1, WHCO5, and WHCO6 cell lines |
濃度 | 400 nM | |
反応時間 | 6 days | |
実験の流れ | Three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit I. Briefly, 1.5 × 103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (antagonist of CXCR2, 400 nM) is added to cells and 0.001% DMSO (solvent) is added as a control. After the indicated incubation period, 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates were left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader. | |
動物実験 | 動物モデル | Rabbits |
投薬量 | 5.5 μg/kg/min | |
投与方法 | Cannula in the external jugular vein |
, , J Cell Mol Med, 2017, 21(7):1411-1419
, , Mol Pain, 2016, doi: 10.1177/1744806916646381
Data from [Data independently produced by , , Theranostics, 2018, 8(5):1270-1285]
Extracellular-vesicle-packaged S100A11 from osteosarcoma cells mediates lung premetastatic niche formation by recruiting gMDSCs [ Cell Rep, 2024, 43(2):113751] | PubMed: 38341855 |
Oncogenic KRASG12D extrinsically induces an immunosuppressive microenvironment in lung adenocarcinoma [ bioRxiv, 2024, 2024.01.16.568090] | PubMed: 38293141 |
PMN-MDSCs modulated by CCL20 from cancer cells promoted breast cancer cell stemness through CXCL2-CXCR2 pathway [ Signal Transduct Target Ther, 2023, 8(1):97] | PubMed: 36859354 |
Tumor Cell-Intrinsic SETD2 Deficiency Reprograms Neutrophils to Foster Immune Escape in Pancreatic Tumorigenesis [ Adv Sci (Weinh), 2023, 10(2):e2202937] | PubMed: 36453584 |
Surgical Treatment of Osteosarcoma Induced Distant Pre-Metastatic Niche in Lung to Facilitate the Colonization of Circulating Tumor Cells [ Adv Sci (Weinh), 2023, 10(28):e2207518] | PubMed: 37585564 |
Surgical Treatment of Osteosarcoma Induced Distant Pre-Metastatic Niche in Lung to Facilitate the Colonization of Circulating Tumor Cells [ Adv Sci (Weinh), 2023, 10(28):e2207518] | PubMed: 37585564 |
Sepsis induces non-classic innate immune memory in granulocytes [ Cell Rep, 2023, 42(9):113044] | PubMed: 37643085 |
A precise molecular subtyping of ulcerative colitis reveals the immune heterogeneity and predicts clinical drug responses [ J Transl Med, 2023, 21(1):466] | PubMed: 37443022 |
Microbial-Dependent Recruitment of Immature Myeloid Cells Promotes Intestinal Regeneration [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007] | PubMed: 37898454 |
Blocking the CXCL1-CXCR2 axis enhances the effects of doxorubicin in HCC by remodelling the tumour microenvironment via the NF-κB/IL-1β/CXCL1 signalling pathway [ Cell Death Discov, 2023, 9(1):120] | PubMed: 37037815 |
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。