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SX-682 {[allProObj[0].p_purity_real_show]}

货号:A1216655

SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.

SX-682 化学结构 CAS号:1648843-04-2
SX-682 化学结构
CAS号:1648843-04-2
SX-682 3D分子结构
CAS号:1648843-04-2
SX-682 化学结构 CAS号:1648843-04-2
SX-682 3D分子结构 CAS号:1648843-04-2
规格 价格 会员价 库存 数量
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SX-682 纯度/质量文件 产品仅供科研

货号:A1216655 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CXCR1 CXCR2 CXCR4 其他靶点 纯度
Reparixin 99%+
SB225002 +++

CXCR2, IC50: 22 nM

99%+
Plerixafor ++

CXCR4, IC50: 44 nM

99%
AMD 3465 6HBr 98%
WZ811 ++++

CXCR4, EC50: 0.3 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

SX-682 生物活性

描述 Recruitment of myeloid-derived suppressor cells (MDSC) into the tumor microenvironment (TME) contributes to cancer immune evasion. MDSCs express the chemokine receptor CXCR2, and inhibiting CXCR2 suppresses the recruitment of MDSCs into the tumor and the premetastatic niche[3]. SX-682, an orally bioavailable small-molecule inhibitor of CXCR1/2 currently undergoing clinical evaluation, could block tumor MDSC recruitment and enhance T cell activation and antitumor immunity following multiple forms of immunotherapy. In mice bearing MOC1 or LLC tumors, SX-682 beginning 10 or 20 days after tumor initiation significantly inhibited trafficking of PMN-MDSCs without altering CXCR2 ligand expression[4]. In mice bearing MOC2 tumors, inhibition of MDSC trafficking with SX-682 (500 mg/kg/day; 1 week) significantly abrogated tumor MDSC accumulation and enhanced the tumor infiltration, activation, and therapeutic efficacy of adoptively transferred murine NK (natural killer) cells[5].

SX-682 参考文献

[1]Sun L, et al. Inhibiting myeloid-derived suppressor cell trafficking enhances T cell immunotherapy. JCI Insight. 2019 Apr 4;4(7).

[2]Lu X, et al. Effective combinatorial immunotherapy for castration-resistant prostate cancer. Nature. 2017 Mar 30;543(7647):728-732.

[3]Yang J, et al. Targeted Deletion of CXCR2 in Myeloid Cells Alters the Tumor Immune Environment to Improve Antitumor Immunity. Cancer Immunol Res. 2021 Feb;9(2):200-213

[4]Sun L, et al. Inhibiting myeloid-derived suppressor cell trafficking enhances T cell immunotherapy. JCI Insight. 2019 Apr 4;4(7):e126853

[5]Greene S, et al. Inhibition of MDSC Trafficking with SX-682, a CXCR1/2 Inhibitor, Enhances NK-Cell Immunotherapy in Head and Neck Cancer Models. Clin Cancer Res. 2020 Mar 15;26(6):1420-1431

SX-682 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.40mL

4.28mL

2.14mL

SX-682 技术信息

CAS号1648843-04-2
分子式C19H14BF4N3O4S
分子量 467.202
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 250 mg/mL(535.1 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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