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Pexidartinib

Cat. No. 7590 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

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 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.

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 Data for Pexidartinib

Solvent Max Conc. mg/mL Max Conc. mM
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.

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

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References for Pexidartinib

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.

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Citations for Pexidartinib

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