SB225002

製品コードS7651 バッチS765103

印刷

化学情報

Chemical Structure 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 (warmed with 50ºC water bath) 16 mg/mL (45.43 mM)
Water 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.
* <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 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] This compound substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. [2] It 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, this compound (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. [4] In addition, it also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models. [5] [6]

プロトコル(参考用のみ)

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

参考

  • https://pubmed.ncbi.nlm.nih.gov/9553055/
  • https://pubmed.ncbi.nlm.nih.gov/16540656/
  • https://pubmed.ncbi.nlm.nih.gov/23611835/
  • https://pubmed.ncbi.nlm.nih.gov/24582495/
  • https://pubmed.ncbi.nlm.nih.gov/19264522/
  • https://pubmed.ncbi.nlm.nih.gov/18653784/

カスタマーフィードバック

, , 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]

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：

Myeloid-Derived Suppressor Cell Accumulation Drives Intestinal Fibrosis through mCCL6/hCCL15 Chemokine-Mediated Fibroblast Activation [ Adv Sci (Weinh), 2025, 12(8):e2411711] PubMed: 39739231
Tumor-derived exosomes induce neutrophil infiltration and reprogramming to promote T-cell exhaustion in hepatocellular carcinoma [ Theranostics, 2025, 15(7):2852-2869] PubMed: 40083930
USP15 Facilitates Colorectal Cancer Immune Evasion through SMYD3/CCL2-Dependent Myeloid-Derived Suppressor Cell Recruitment [ Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194] PubMed: 40323348
Cholesterol 25-Hydroxylase Enhances Myeloid-Derived Suppressor Cell (MDSC) Immunosuppression via the Stimulator of Interferon Genes (STING)-Tank-Binding Kinase 1 (TBK1)-Receptor-Interacting Protein Kinase 3 (RIPK3) Pathway in Colorectal Cancer [ MedComm (2020), 2025, 6(10):e70411] PubMed: 41020041
CXCR2 mediates rotenone-induced neuroinflammation and neurodegeneration through neurotrophil infiltration and extracellular traps formation in mice [ Int J Biol Macromol, 2025, 330(Pt 4):148305] PubMed: 41093199
KRASG12D drives immunosuppression in lung adenocarcinoma through paracrine signaling [ JCI Insight, 2025, 10(1)e182228] PubMed: 39782689
Induction of cell death by the CXCR2 antagonist SB225002 in colorectal cancer and stromal cells [ Biomed Pharmacother, 2025, 188:118203] PubMed: 40412356
The crosstalk of monocyte-neutrophil in hair follicles regulates neutrophil transepidermal migration in contact dermatitis [ Commun Biol, 2025, 8(1):564] PubMed: 40185981
IDO1 promotes Echinococcus multilocularis infection by regulating the formation of neutrophil extracellular traps [ Vet Res, 2025, 56(1):131] PubMed: 40597301
Extracellular-vesicle-packaged S100A11 from osteosarcoma cells mediates lung premetastatic niche formation by recruiting gMDSCs [ Cell Rep, 2024, 43(2):113751] PubMed: 38341855

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。

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