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编 号：F323708
分子式：C15H14ClFN4O2S2
分子量：400.88
分子式：C15H14ClFN4O2S2
分子量：400.88
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CAS No: 333742-63-5
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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.
体内研究：
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。 AZ10397767 (化合物 30a) 在大鼠中的 CL 为 4 ml/min/kg。 Animal Model:SCID mice with A549 cells
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.
体外研究：
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。 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。 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。
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.
体内研究：
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。 AZ10397767 (化合物 30a) 在大鼠中的 CL 为 4 ml/min/kg。 Animal Model:SCID mice with A549 cells
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.
体外研究：
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。 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。 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。
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