SX-682 是口服有效的CXCR1和CXCR2变构抑制剂，可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫，具有治疗去势抵抗性前列腺癌的潜力。

SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

SX-682 significantly inhibited trafficking of PMN-MDSCs without altering CXCR2 ligand expression.?Trafficking of CXCR1+ macrophages was unaltered, possibly due to coexpression of CSF1R.?Reduced PMN-MDSC tumor infiltration correlated with enhanced accumulation of endogenous or adoptively transferred T cells.?Accordingly, tumor growth inhibition or the rate of established tumor rejection following programed death-axis (PD-axis) immune checkpoint blockade or adoptive cell transfer of engineered T cells was enhanced in combination with SX-682.

1648843-04-2

C19H14BF4N3O4S

467.2

DMSO:250 mg/mL (535.10 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years