AZ 10397767

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Cat.No. 5872 - AZ 10397767 | C15H14ClFN4O2S2 | CAS No. 333742-63-5
Description: Potent CXCR2 antagonist
Chemical Name: 5-[[(3-Chloro-2-fluorophenyl)methyl]thio]-7-[[(1R)-2-hydroxy-1-methylethyl]amino]thiazolo[4,5-d]pyrimidin-2(3H)-one
Purity: ≥98% (HPLC)

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 333742-63-5
PubChem ID 11858154
Smiles C[C@@H](NC1=C2SC(NC2=NC(SCC3=C(C(Cl)=CC=C3)F)=N1)=O)CO

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 40.09 100

Preparing Stock Solutions

The following data is based on the product molecular weight 400.88. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.49 mL 12.47 mL 24.95 mL
5 mM 0.5 mL 2.49 mL 4.99 mL
10 mM 0.25 mL 1.25 mL 2.49 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Safety Datasheet


References are publications that support the products' biological activity.

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

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

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

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