Pexidartinib

Product Description

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 BRAF^V600E-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.

Solubility

Preparing Stock Solutions for Pexidartinib

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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	1.20 mL	2.39 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Mok Inhibition of CSF-1 receptor improves the antitumor efficacy of adoptive cell transfer immunotherapy. Cancer Res. 2014 PMID: 24247719
• Sluijter Inhibition of CSF-1R supports T-cell mediated melanoma therapy. PLoS One. 2014 PMID: 25110953
• DeNardo Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 PMID: 22039576