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SX-682

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Chemical Structure| 1648843-04-2 同义名 : -
CAS号 : 1648843-04-2
货号 : A1216655
分子式 : C19H14BF4N3O4S
纯度 : 99%+
分子量 : 467.202
MDL号 : MFCD28502254
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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