AZ10397767

CAS: 333742-63-5 F: C15H14ClFN4O2S2 W: 400.88

AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxal

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Bioactivity	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].
Invitro	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]。 Cell Proliferation Assay[2] Cell Line:
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]。 Animal Model:
Name	AZ10397767
CAS	333742-63-5
Formula	C15H14ClFN4O2S2
Molar Mass	400.88
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Iain Walters, et al. Evaluation of a series of bicyclic CXCR2 antagonists. Bioorg Med Chem Lett. 2008 Jan 15;18(2):798-803. [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. [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. [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.

7-Oxostaurosporine