2. GPCR/G Protein Immunology/Inflammation
  3. CXCR
  4. AZ10397767

AZ10397767 是一种具有口服活性的、选择性 CXCR2 受体拮抗剂，IC50 为 1 nM。AZ10397767 减弱 Oxaliplatin (HY-17371) 诱导的 NF-κB 转录活性并增强 Oxaliplatin 诱导的雄激素非依赖性前列腺癌 (AIPC) 细胞凋亡。AZ10397767 显着抑制中性粒细胞募集到肿瘤中，从而在体外和体内对肿瘤生长产生不利影响。

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AZ10397767 Chemical Structure

AZ10397767 Chemical Structure

CAS No. : 333742-63-5

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规格 价格 是否有货 数量
5 mg ￥3941
3 - 4 周
10 mg 现货 3 - 4 周
50 mg   询价  
100 mg   询价  

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AZ10397767 相关抗体

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

CXCR2

1 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
1 nM
Compound: 30a
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
[PMID: 18240390]
体外研究
(In Vitro)

AZ10397767 (20 nM; 48小时) 消除 IL-8 (3 nM) 诱导的细胞增殖，将细胞数量减少至基础水平以下[2]。
AZ10397767 (20 nM; 72小时) 增加 Oxaliplatin (HY-17371) 的细胞毒性，并增强 Oxaliplatin 诱导的 AIPC 细胞凋亡。AZ10397767 本身不能诱导 PC3 或 DU145 细胞凋亡[3]。
AZ10397767 (20 nM; 24小时) 减弱 Oxaliplatin 诱导的 NF-κB 转录活性，减弱 PC3 和 DU145 细胞中每种 CXC 趋化因子 (CXCL8 和 CXCL1) 和抗凋亡基因 (Bcl-2 和生存素) 的 mRNA 转录水平的增加[3]。

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

AZ10397767 相关抗体:

Cell Proliferation Assay[2]

Cell Line: LNCaP cells and 22Rv1 cells
Concentration: 20 nM
Incubation Time: 48 h
Result: Abrogated the IL-8-induced (3 nM) increase in proliferation, reducing cell number to below basal levels.

Apoptosis Analysis[3]

Cell 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-PCR[3]

Cell 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.
体内研究
(In Vivo)

AZ10397767 (100 mg/kg; 口服灌胃; 每天两次; 持续 22 天) 在 A549 异种移植肿瘤中表现出中性粒细胞浸润减少并伴有肿瘤生长迟缓[4]。
AZ10397767 (化合物 30a) 在大鼠中的 CL 为 4 ml/min/kg[1]。

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

Animal Model: SCID mice with A549 cells[4]
Dosage: 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.
分子量

400.88

Formula

C15H14ClFN4O2S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AZ10397767 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ10397767333742-63-5AZ 10397767AZ-10397767CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsNF-κB transcriptionalandrogen-independent prostate cancerAIPCneutrophiltumorLNCaP22Rv1A549Inhibitorinhibitorinhibit

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目录号：
HY-124056
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