Pexidartinib
Chemical Name: N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
Purity: ≥98%
Biological Activity
Pexidartinib is a potent colony-stimulating factor-1 receptor (CSF-1R) tyrosine kinase inhibitor (IC50 = 20 nM). In the B16F10 mouse melanoma model, Pexidartinib reduces the systemic and local accumulation of macrophages without affecting Gr-1+ myeloid derived suppressor cells. When combined with tumor-specific CD8 T cell immunotherapy, Pexidartinib promotes the control of tumor growth. In the BRAFV600E-driven mouse melanoma model, Pexidartinib improves the efficacy of adoptive cell therapy with reduction of TIMs and an increase in tumor-infiltrating lymphocytes and T cells. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Leukocyte Complexity Predicts Breast Cancer Survival and Functionally Regulates Response to Chemotherapy.
Denardo DG, Brennan DJ, Rexhepaj E, Ruffell B, Shiao SL et al.
Cancer Discov;1(1):54-67.
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