Pexidartinib (1029044-16-3) is a potent and selective dual inhibitor of CSF1R (IC50 = 20nM) and c-KIT (IC50 = 10nM).1 Inhibition of CSF1R with Pexidartinib resulted in a reprogrammed immune microenvironment that fosters antitumor immunity in a CD8+ T-cell-dependent manner in a breast cancer model.1 CSF1R recruits tumor-infiltrating myeloid cell that suppress tumor immunity - Pexidartinib increased the efficacy of adoptive cell immunotherapy (ACT) in a mouse melanoma model by inhibiting the intratumoral accumulation of immunosuppressive macrophages.2,3 It has also been shown to increase the efficacy of anti-PD-14,5 and DC immunotherapy 6.
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