AZ10397767 

AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC₅₀ of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo^[1][2][3][4].

AZ10397767 (20 nM; 48 h) abrogates the IL-8-induced (3 nM) increase in proliferation, reducing cell number to below basal levels^[2].
AZ10397767 (20 nM; 72 h) increases Oxaliplatin (HY-17371) cytotoxicity, and potentiates Oxaliplatin-induced apoptosis in AIPC cells. AZ10397767 by itself fails to induce apoptosis in either PC3 or DU145 cells^[3].
AZ10397767 (20 nM; 24 h) attenuates the Oxaliplatin-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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZ10397767 (100 mg/kg; Orally; twice daily; for 22 days) display reduced neutrophil infiltration accompanied with retardation in tumor growth in A549 xenograft tumors^[4].
AZ10397767 (compound 30a) has a CL of 4 ml/min/kg in rat^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

400.88

C₁₅H₁₄ClFN₄O₂S₂

333742-63-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Iain Walters, et al. Evaluation of a series of bicyclic CXCR2 antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):798-803.  [Content Brief]

  [2]. Angela Seaton, et al. Interleukin-8 signaling promotes androgen-independent proliferation of prostate cancer cells via induction of androgen receptor expression and activation. Carcinogenesis. 2008 Jun;29(6):1148-56.  [Content Brief]

  [3]. Catherine Wilson, et al. 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. 2008 Dec;327(3):746-59.  [Content Brief]

  [4]. Simon Tazzyman, et al. 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. 2011 Aug 15;129(4):847-58.  [Content Brief]