AZ 10397767

Names

[ Name ]:
AZ 10397767

[Synonym ]:
5-[(3-chloro-2-fluorobenzyl)sulfanyl]-7-{[(2R)-1-hydroxypropan-2-yl]amino}[1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one
Thiazolo[4,5-d]pyrimidin-2(3H)-one, 5-[[(3-chloro-2-fluorophenyl)methyl]thio]-7-[[(1R)-2-hydroxy-1-methylethyl]amino]-
5-[(3-Chloro-2-fluorobenzyl)sulfanyl]-7-{[(2R)-1-hydroxy-2-propanyl]amino}[1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one

Biological Activity

[Description]:

AZ10397767 is a potent, selective CXCR2 inhibitor that inhibits CXCL8 binding to CXCR2 with pIC50 of 9.0; weakly inhibits CXCL8 binding to CXCR1 with pIC50<7, and no affinity for CCR2 and CCR5; significantly attenuates IL-8-induced c-FLIP mRNA up-regulation whereas inhibition of AR- and/or NF-kappaB-mediated transcription attenuated IL-8-induced c-FLIP expression in LNCaP and PC3 cells, respectively; attenuates oxaliplatin-induced NF-kappaB activation, increases oxaliplatin cytotoxicity, and potentiates oxaliplatin-induced apoptosis in AIPC cells.

[References]

References 1. Wilson C, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):746-59. 2. Seaton A, et al. Carcinogenesis. 2008 Jun;29(6):1148-56. 3. Wilson C, et al. Mol Cancer Ther. 2008 Sep;7(9):2649-61. 4. Walters I, et la. Bioorg Med Chem Lett. 2008 Jan 15;18(2):798-803. View Related Products by Target Chemokine Receptor (CCR and CXCR)

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C₁₅H₁₄ClFN₄O₂S₂

[ Molecular Weight ]:
400.879

[ Exact Mass ]:
400.023071

[ LogP ]:
5.03

[ Index of Refraction ]:
1.708

Related Compounds

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