SB225002

Catalog No.S7651 Batch:S765104

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Technical Data

Formula

C13H10BrN3O4
Molecular Weight 352.14 CAS No. 182498-32-4
Solubility (25°C)* In vitro DMSO 70 mg/mL (198.78 mM)
Ethanol 18 mg/mL (51.11 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50%ddH2O
5.0mg/ml 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; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 2 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
CXCR2 [1]
(Cell-free assay)
22 nM
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Assay:[2]
  • Cell lines

    WHCO1, WHCO5, and WHCO6 cell lines

  • Concentrations

    400 nM

  • Incubation Time

    6 days

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Rabbits

  • Dosages

    5.5 μg/kg/min

  • Administration

    Cannula in the external jugular vein

Customer Product Validation

, , 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]

Data from [Data independently produced by , , Oncogene, 2017, 36(15):2095-2104]

Selleck's SB225002 has been cited by 80 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.