AZ 10397767

Cat. No. 5872new

AZ 10397767 C15H14ClFN4O2S2 [333742-63-5]

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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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Tazzyman et al (2011) Inhibition of neutrophil infiltration into A549 lung tumors in vitro and in vivo using a CXCR2-specific antagonist is associated with reduced tumor growth. Int.J.Cancer 129 847. PMID: 21328342.

Walters et al (2008) Evaluation of a series of bicyclic CXCR2 antagonists. Bioorg.Med.Chem.Lett. 18 798. PMID: 18240390.

Wilson et al (2008) 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. J.Pharmacol.Exp.Ther. 327 746. PMID: 18780829.

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Keywords: AZ 10397767, supplier, AZ10397767, chemokine, cxc, receptors, antagonists, antagonism, orally, bioavailable, potent, selective, Tocris Bioscience, Chemokine CXC Receptor Antagonist products

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