UNC2025

10/01/2018 - "Pharmacokinetic studies showed high tumor exposures of UNC2025 in a syngeneic orthotopic allograft mouse GBM model. "
10/01/2018 - "UNC2025 also reduced CD206+ macrophages in mouse tumor samples. "
01/01/2016 - "Thus, UNC2025 mediates anti-tumor activity in GBM by multiple mechanisms. "
01/01/2019 - "In patient-derived melanoma xenograft models, treatment with UNC2025 blocked or significantly reduced tumor growth. "
01/01/2021 - "Functional assays in MerTK-high and MerTK-deficient cells further demonstrate that the anti-cancer efficacy of UNC2025 is MerTK-independent. "

03/15/2017 - "Approximately 30% of primary leukemia patient samples (78 of 261 total) were sensitive to UNC2025. "
03/15/2017 - " Design: Preclinical in vitro and in vivo assays using cell lines and primary leukemia patient samples were used to evaluate antileukemic effects of UNC2025.Results: UNC2025 potently inhibited prosurvival signaling, induced apoptosis, and reduced proliferation and colony formation in MERTK-expressing ALL and AML cell lines and patient samples. "
03/15/2017 - ": The broad-spectrum activity mediated by UNC2025 in leukemia patient samples and xenograft models, alone or in combination with cytotoxic chemotherapy, supports continued development of MERTK inhibitors for treatment of leukemia. "
03/15/2017 - "Here, we evaluated the utility of UNC2025, a MERTK tyrosine kinase inhibitor, for treatment of acute leukemia.Experimental"
03/15/2017 - "UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models."

01/01/2018 - "UNC2025 decreases platelet activation in vitro and thrombus formation in vivo. "
01/01/2018 - "The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis."
01/01/2018 - "Results and Conclusions Treatment with UNC2025 inhibited MERTK phosphorylation and downstream activation of AKT and SRC, decreased platelet activation, and protected animals from pulmonary embolism and arterial thrombosis without increasing bleeding times. "

01/01/2018 - "Results and Conclusions Treatment with UNC2025 inhibited MERTK phosphorylation and downstream activation of AKT and SRC, decreased platelet activation, and protected animals from pulmonary embolism and arterial thrombosis without increasing bleeding times. "

01/01/2019 - "In patient-derived melanoma xenograft models, treatment with UNC2025 blocked or significantly reduced tumor growth. "
01/01/2019 - "In melanoma cell lines, treatment with UNC2025 potently inhibited phosphorylation of MERTK and downstream signaling, induced cell death, and decreased colony formation. "
01/01/2019 - "Here we report the effect of treatment with a MERTK-selective small molecule inhibitor, UNC2025, in preclinical models of melanoma. "
01/01/2019 - "These data support the use of UNC2025 for treatment of melanoma, irrespective of BRAF or NRAS mutational status, and suggest a role for MERTK and targeted combination therapy in BRAF and NRAS-mutated melanoma."