Catalog Number: 5872
Chemical Name: 5-[[(3-Chloro-2-fluorophenyl)methyl]thio]-7-[[(1R)-2-hydroxy-1-methylethyl]amino]thiazolo[4,5-d]pyrimidin-2(3H)-one
Biological Activity
Potent CXCR2 antagonist (IC50 = 1 nM); attenuates oxaliplatin-induced NF-κB activation, increases oxaliplatin cytotoxicity, and potentiates oxaliplatin-induced apoptosis in AIPC cells. Reduces the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models. Orally bioavailable.
Technical Data
  • M.Wt:
    400.88
  • Formula:
    C15H14ClFN4O2S2
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    333742-63-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Chemotherapy-induced CXC-chemokine/CXC-chemokine receptor signaling in metastatic prostate cancer cells confers resistance to oxaliplatin through potentiation of nuclear factor-kappaB transcription and evasion of apoptosis.
    Wilson et al.
    J.Pharmacol.Exp.Ther., 2008;327:746
  2. Evaluation of a series of bicyclic CXCR2 antagonists.
    Walters et al.
    Bioorg.Med.Chem.Lett., 2008;18:798
  3. Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth.
    Tazzyman et al.
    Int.J.Cancer, 2011;129:847
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