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Chemical Structure| 182498-32-4 Chemical Structure| 182498-32-4

Structure of SB225002
CAS No.: 182498-32-4

Chemical Structure| 182498-32-4

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SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM, showing > 150-fold selectivity over CXCR1 and four other 7-TMRs.

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Product Details of SB225002

CAS No. :182498-32-4
Formula : C13H10BrN3O4
M.W : 352.14
SMILES Code : O=C(NC1=CC=C([N+]([O-])=O)C=C1O)NC2=CC=CC=C2Br
MDL No. :MFCD00954637
InChI Key :MQBZVUNNWUIPMK-UHFFFAOYSA-N
Pubchem ID :3854666

Safety of SB225002

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SB225002

GPCR

Isoform Comparison

Biological Activity

Target
  • CXCR2

    CXCR2, IC50:22 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
bone marrow-derived MDSCs 2 μM 4 days to eliminate the effect of CXCL1 on the generation of MDSCs Acta Pharm Sin B. 2023 Dec;13(12):4733-4747.
U937-derived macrophages 1 µM 12 h To evaluate the effect of SB225002 on macrophage invasiveness, results showed that SB225002 significantly inhibited MTD-CAFs-induced macrophage invasion. J Exp Med. 2016 Dec 12;213(13):2967-2988.
BC-011 carcinoma cells 1 µM 5 days To evaluate the effect of SB225002 on the proportion of CD44+CD24low/− TICs, results showed that SB225002 significantly reduced the MTD-CAFs-induced increase in CD44+CD24low/− TICs. J Exp Med. 2016 Dec 12;213(13):2967-2988.
BM-MSCs 200 nM 24 h SB225002 was used to inhibit the GRO-α receptor, reducing the migration of BM-MSCs towards OS cells. Mol Oncol. 2018 May;12(5):659-676.
HOS cells 200 nM 24 h SB225002 was used to inhibit the GRO-α receptor, reducing the invasion and transendothelial migration of HOS cells. Mol Oncol. 2018 May;12(5):659-676.
C4-2B 50 nM 30 min To investigate the effect of SB225002 on the migration of C4-2B cells, results showed that SB225002 had no significant effect on the migration of C4-2B cells Int J Mol Sci. 2021 Feb 17;22(4):1994.
PC-3 50 nM 30 min To investigate the effect of SB225002 on the migration of PC-3 cells, results showed that SB225002 had no significant effect on the migration of PC-3 cells Int J Mol Sci. 2021 Feb 17;22(4):1994.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Experimental Autoimmune Encephalomyelitis (EAE) Intraperitoneal injection 0.1 mg/kg Daily for 20 days SB225002 significantly ameliorated EAE in ELT mice. Nat Commun. 2021 Jan 4;12(1):105
Mice G422 glioma model Intraperitoneal injection 10 mg/kg Daily for 14 days To inhibit CXCL1 signaling, reduce MDSC accumulation, and slow tumor growth Acta Pharm Sin B. 2023 Dec;13(12):4733-4747.
B6C3F1 mice Subcutaneous ovarian cancer model Intraperitoneal injection 1 mg/kg Twice a week, until the end of the experiment SB225002 retarded tumour growth by inhibiting CXCR2 signaling and increased the activity of CD8+ T cells. Br J Cancer. 2020 Oct;123(9):1404-1416
Mice Type-B EAE model Intraperitoneal injection 0.1 mg/kg Once daily for 20 days SB225002 significantly ameliorated Type-B EAE but had no effect on Type-A EAE. Nat Neurosci. 2016 Dec;19(12):1599-1609
NOG mice Mammary fat pad tumor model Intraperitoneal injection 0.5 mg/kg Daily, throughout the treatment cycle To evaluate the effect of SB225002 on tumor growth and the proportion of CD44+CD24low/? TICs, results showed that SB225002 significantly inhibited MTD-CAFs-induced tumor growth and the increase in CD44+CD24low/? TICs. J Exp Med. 2016 Dec 12;213(13):2967-2988.
Mice RMA tumor model Intraperitoneal injection 0.8 mM Every 2 days until the end of the experiment To study the effect of SB225002 on RMA tumor growth J Exp Med. 2013 Aug 26;210(9):1711-28.
Mice B16-F10 melanoma model Intraperitoneal injection 2 mg/kg Daily until the end of the experiment Inhibited HFHCD-induced tumor growth acceleration by blocking myeloid cell migration into the tumor Nat Commun. 2022 Sep 14;13(1):5399

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.20mL

2.84mL

1.42mL

28.40mL

5.68mL

2.84mL

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