Pexidartinib, CSF1R inhibitor (TBI4829)

Description

Product Details

Formal Name: 5-[(5-Chloro-1H-pyrrolo[2,3.b]pyridine-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine

Alternate Names: PLX3397

Molecular Formula: C₂₀H₁₅ClF₃N₅

Formula Weight: 417.81

CAS Number: 1029044-16-3

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 10 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

CSF1R inhibitor

Functions

Pexidartinib (1029044-16-3) is a potent and selective dual inhibitor of CSF1R (IC50 = 20nM) and c-KIT (IC50 = 10nM). Inhibition of CSF1R with Pexidartinib resulted in a reprogrammed immune microenvironment that fosters antitumor immunity in a CD8+ T-cell-dependent manner in a breast cancer model.1 CSF1R recruits tumor-infiltrating myeloid cell that suppress tumor immunity – Pexidartinib increased the efficacy of adoptive cell immunotherapy (ACT) in a mouse melanoma model by inhibiting the intratumoral accumulation of immunosuppressive macrophages. It has also been shown to increase the efficacy of anti-PD-1 and DC immunotherapy.

Application Procedures

First dissolved in DMSO (up to at least 10 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.