biostudies-literatureSynn CBNational Research Foundation of Koreae1364https://www.ebi.ac.uk/biostudies/studies/S-EPMC8716998biostudies-literatureUnknown11(1)<h4>Objectives</h4>AXL-mediated activation of aberrant tyrosine kinase drives various oncogenic processes and facilitates an immunosuppressive microenvironment. We evaluated the anti-tumor and anti-metastatic activities of SKI-G-801, a small-molecule inhibitor of AXL, alone and in combination with anti-PD-1 therapy.<h4>Methods</h4><i>In vitro</i> pAXL inhibition by SKI-G-801 was performed in both human and mouse cancer cell lines. Immunocompetent mouse models of tumor were established to measure anti-metastatic potential of SKI-G-801. Furthermore, SKI-G-801, anti-PD-1 or their combination was administered as an adjuvant or neoadjuvant in the 4T1 tumor model to assess their potential for clinical application.<h4>Results</h4>SKI-G-801 robustly inhibited pAXL expression in various cell lines.Clinical & translational immunologySKI-G-801, an AXL kinase inhibitor, blocks metastasis through inducing anti-tumor immune responses and potentiates anti-PD-1 therapy in mouse cancer models.PMC87169982017R1D1A1B0303211014Yun JKim CGLee SLim SChoi HPyo KHYun MRKim SECho BCSynn CBKim MHLee HKLee JMChoi YHeo SGKim YSCho JSKim DHLim SMJo HNKim DKPark SAhn BCKim HRHong MHLee EJKim JHPark CWLee SSLee YWLee WYang SDByeon YfalseSKI-G-801, an AXL kinase inhibitor, blocks metastasis through inducing anti-tumor immune responses and potentiates anti-PD-1 therapy in mouse cancer models.<h4>Objectives</h4>AXL-mediated activation of aberrant tyrosine kinase drives various oncogenic processes and facilitates an immunosuppressive microenvironment. We evaluated the anti-tumor and anti-metastatic activities of SKI-G-801, a small-molecule inhibitor of AXL, alone and in combination with anti-PD-1 therapy.<h4>Methods</h4><i>In vitro</i> pAXL inhibition by SKI-G-801 was performed in both human and mouse cancer cell lines. Immunocompetent mouse models of tumor were established to measure anti-metastatic potential of SKI-G-801. Furthermore, SKI-G-801, anti-PD-1 or their combination was administered as an adjuvant or neoadjuvant in the 4T1 tumor model to assess their potential for clinical application.<h4>Results</h4>SKI-G-801 robustly inhibited pAXL expression in various cell lines.2022-01-01T00:00:00Z20222026-05-09T11:57:02.114Z2022-02-11T15:07:21.754ZS-EPMC87169983500374810.1002/cti2.1364