Pexidartinib

Name: Pexidartinib
Brand: Tocris Bioscience
SKU: 7590

Tocris Bioscience, part of Bio-Techne | Catalog # 7590

Citations (2)

COA / SDS

Potent CSF-1R inhibitor

Key Product Details

Description:	Potent CSF-1R inhibitor
Chemical Name:	N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine
Purity:	≥98% (HPLC)
Molecular Weight:	417.82

View Full Technical Details for Pexidartinib

Technical Data
Citations

Biological Activity for Pexidartinib

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.

Compound Libraries for Pexidartinib

Pexidartinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Pexidartinib

M. Wt	417.82
Formula	C₂₀H₁₅ClF₃N₅
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1029044-16-3
PubChem ID	25151352
InChi Key	JGWRKYUXBBNENE-UHFFFAOYSA-N
Smiles	ClC1=CC2=C(N=C1)NC=C2CC(C=C3)=CN=C3NCC(C=C4)=CN=C4C(F)(F)F

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.

Solubility for Pexidartinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	41.78	100

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

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References for Pexidartinib

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