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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.
Pexidartinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 417.82. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.39 mL||11.97 mL||23.93 mL|
|5 mM||0.48 mL||2.39 mL||4.79 mL|
|10 mM||0.24 mL||1.2 mL||2.39 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the biological activity of the product.
DeNardo et al (2011) Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 1 54 PMID: 22039576
Mok et al (2014) Inhibition of CSF-1 receptor improves the antitumor efficacy of adoptive cell transfer immunotherapy. Cancer Res. 74 153 PMID: 24247719
Sluijter et al (2014) Inhibition of CSF-1R supports T-cell mediated melanoma therapy. PLoS One. 9 e104230 PMID: 25110953
If you know of a relevant reference for Pexidartinib, please let us know.
Keywords: Pexidartinib, Pexidartinib supplier, potent, receptor, tyrosine, kinases, inhibitors, inhibits, colony-stimulating, factor-1, CSF-1R, CSF1R, Other, RTKs, 7590, Tocris Bioscience
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