AZ 10397767

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZ10397767 是一种有效的选择性 CXCR2 抑制剂，可抑制 CXCL8 与 CXCR2 的结合，pIC50 为 9.0。

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.

Cell Proliferation Assay Cell Line:LNCaP cells and 22Rv1 cells Concentration:20 nM Incubation Time:48 hResult:Abrogated the IL-8-induced (3 nM) increase in proliferation, reducing cell number to below basal levels.Apoptosis AnalysisCell Line:PC3 or DU145 cells Concentration:20 nM Incubation Time:72 h Result:Coadministration with 0.1 or 1 μM Oxaliplatin resulted in a marked increase in the sub-G0/G1 cell population in either cell line.Potentiates Oxaliplatin-induced apoptosis in AIPC cells.RT-PCRCell Line:PC3 or DU145 cells Concentration:20 nM Incubation Time:24 h Result:Attenuated the Oxaliplatin (1 μM)-induced NF-κB transcriptional activity and the increases in mRNA transcript levels for each of the CXC-chemokines (CXCL8 and CXCL1) and antiapoptotic genes (Bcl-2 and survivin) in the PC3 and DU145 cells.

Animal Model:SCID mice with A549 cellsDosage:100 mg/kg Administration:Orally; twice daily; for 22 days Result:Tumors were 36% smaller than their control counterparts. Significantly (p < 0.01) reduced the number of tumor-infiltrating neutrophils compared to mice receiving vehicle control.

AZ10397767 | AZ-10397767 | AZ767 | AZ 767

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

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333742-63-5

400.871

C15H14ClFN4O2S2

>98% (HPLC)

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O=C1SC2=C(N[C@H](C)CO)N=C(SCC3=CC=CC(Cl)=C3F)N=C2N1

(1R)-5-[[(3-chloro-2-fluorophenyl)methyl]thio]-7-[[2-hydroxy-1-methylethyl]amino]thiazolo[4,5-d]pyrimidin-2(3H)-one

(-20℃)

With Ice Pack

≥ 2 years