SB 225002

Katalognr.S7651 Batch:S765104

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Tekniska data

Formel

C13H10BrN3O4
Molekylvikt 352.14 CAS-nr. 182498-32-4
Löslighet (25°C)* In vitro DMSO 70 mg/mL (198.78 mM)
Ethanol 18 mg/mL (51.11 mM)
Water Insoluble
In Vivo (Tillsätt lösningsmedel till produkten individuellt och i ordning.)
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 40%PEG 300 5%Tween80 50%ddH2O

Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.

 5.000mg/ml (14.20mM) 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

Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.

 0.100mg/ml (0.28mM) 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 betyder svårlösligt eller olösligt.
* Vänligen notera att Selleck testar lösligheten för alla förbindelser internt, och den faktiska lösligheten kan skilja sig något från publicerade värden. Detta är normalt och beror på små variationer mellan olika partier.
* Rumstempererad frakt (Stabilitetstester visar att denna produkt kan fraktas utan några kylåtgärder.)

Beredning av stamlösningar

Biologisk aktivitet

Beskrivning SB225002 är en potent och selektiv CXCR2-antagonist med ett IC50-värde på 22 nM för hämning av interleukin IL-8-bindning till CXCR2, med > 150 gånger högre selektivitet än för övriga testade 7-TMR.
Mål
CXCR2
(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. This compound substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. It also shows the antitumor activity as a microtubule inhibitor.
In Vivo In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. In mouse intrahepatic cholangiocellular carcinoma model, this compound (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. In addition, it also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models.

Protokoll (från referens)

Kinasanalys:[1]
  • Radioligandbindningsförsök

    Analyserna utförs i 96-brunnsmikrotiterplattor där reaktionsblandningen innehåller 1,0 μg/ml membranprotein i 20 mM Bis-Tris-propan, pH 8,0, med 1,2 mM MgSO4, 0,1 mM EDTA, 25 mM NaCl och 0,03% CHAPS samt SB 225002 (10 mM stam-lösning i Me2SO) tillsatt i de angivna koncentrationerna; den slutliga Me2SO-koncentrationen är <1% under standardbindningsförhållanden. Bindningen initieras genom tillsats av 0,25 nM 125I-IL-8 (2 200 Ci/mmol). Efter 1 timmes inkubering vid rumstemperatur skördas plattan med en Tomtec 96-brunnsskördare på en glasfibersfiltermatta blockerad med 1% polyetylenimin, 0,5% BSA och tvättas tre gånger med 25 mM NaCl, 10 mM Tris·HCl, 1 mM MgSO4, 0,5 mM EDTA, 0,03% CHAPS, pH 7,4. Filtret torkas, förseglas i en provpåse innehållande 10 ml Wallac 205 Betaplate vätskescintillationsvätska och räknas med en Wallac 1205 Betaplate vätskescintillationsräknare.
Cellanalys:[2]
  • Cellinjer

    WHCO1, WHCO5, and WHCO6 cell lines

  • Koncentrationer

    400 nM

  • Inkubationstid

    6 days

  • Metod

    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.
Djurstudie:[1]
  • Djurmodeller

    Rabbits

  • Doseringar

    5.5 μg/kg/min

  • Administrering

    Cannula in the external jugular vein

Referenser

  • 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/

Kundvalidering av produkt

<p>SB225002 could inhibited h-JBMMSCs chemotaxis in both the co-culture and the monoculture transwell systems (n = 3; *P < 0.05).</p>

, , J Cell Mol Med, 2017, 21(7):1411-1419

<p>(e, f) Administration of the selective CXCR2 antagonist SB225002 mitigated mechanical hyperalgesia and heat hyperalgesia in CCI rats. Antinociceptive effects of a single intrathecal (it.) injection of 20 µg SB225002 were observed at 1 h and disappeared at 2 h. Antinociceptive effects induced by a single injection of SB225002 at 40 µg were observed at 1 h and disappeared 6 h after injection. Injection of SB225002 (10 µg, i.t.) did not alter the PWT and PWL of CCI rats. N = 6 rats for each group, *p < .05, compared to NS group. PWL: paw withdraw latency; PWT: paw mechanical withdrawal thresholds.</p>

, , Mol Pain, 2016, doi: 10.1177/1744806916646381

(G) Concentration-dependent inhibition of cell proliferation in SKOV3 cells (* P ≤ 0.005) treated with SB225002 (0.625, 1.25, 2.5 and 5 μM) for 2 days was revealed using XTT cell proliferation assay. (H) Western blot analysis confirmed that TAK1/NFκB signaling was inhibited dose-dependently in SKOV3 cells upon treatment with SB225002 (1.25 and 2.5 μM) as compared with untreated control.

Data från [ , , Theranostics, 2018, 8(5):1270-1285 ]

The inhibitor SB225002 significantly decreased J82-, CXCL2- or MIF-mediated MDSC migration. The bars represent the s.e.m. of three experiments. *P<0.05.

Data från [ , , Oncogene, 2017, 36(15):2095-2104 ]

Sellecks SB 225002 Har citerats av 91 Publikationer

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

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