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.
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- CAS. Nr.: 333742-63-5
- Formel: C15H14ClFN4O2S2
- Molecular Weight:400.88
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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CXCR2 1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
1 nM
Compound: 30a
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Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
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[PMID: 18240390] |
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.
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Cell Line:LNCaP cells and 22Rv1 cells
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Concentration:20 nM
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Incubation Time:48 h
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Result:Abrogated the IL-8-induced (3 nM) increase in proliferation, reducing cell number to below basal levels.
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Cell Line:PC3 or DU145 cells
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Concentration:20 nM
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Incubation Time:72 h
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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.
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Cell Line:PC3 or DU145 cells
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Concentration:20 nM
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Incubation Time:24 h
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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.
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.
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Animal Model:SCID mice with A549 cells[4]
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Dosage:100 mg/kg
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Administration:Orally; twice daily; for 22 days
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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.
Chemical Information
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CAS. Nr. 333742-63-5
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Molecular Weight 400.88
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Formel C15H14ClFN4O2S2
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SMILES
O=C1SC2=C(N[C@H](C)CO)N=C(SCC3=CC=CC(Cl)=C3F)N=C2N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AZ10397767 Related Classifications
HY-124056 Related Classifications
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