Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively.
In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.
Cancer Lett. 2022 Feb 28;527:174-190.
Hippo/YAP Signaling Choreographs The Tumor Immune Microenvironment to Promote Triple Negative Breast Cancer Progression Via TAZ/IL-34 Axis
Pexidartinib purchased from AbMole
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Source | (2021). Figure 7. Pexidartinib (Abmole Bioscience, USA) |
| Method | tumor growth and metastasis assay | |
| Cell Lines | xenograft tumor growth model | |
| Concentrations | 40 mg/kg | |
| Incubation Time | 5 days every week | |
| Results | As expected, we observed a significant reduction in TAMs in the pexidartinib plus anti-PD-L1 treatment group and an increased number of CD8+ T cells in the combined treatment group (Fig. 7F, 7H, S9A and S9C). Immunofluorescence staining further validated the increase in the number of intratumoral CD8+ T cells in the combined treatment group (Fig. 7G and S9B) |
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Source | (2021). Figure 4. Pexidartinib (Abmole Bioscience, USA) |
| Method | tumor growth and metastasis assay | |
| Cell Lines | xenograft tumor growth model | |
| Concentrations | 40 mg/kg | |
| Incubation Time | 5 days every week | |
| Results | The phospho-kinase array and WB indicated that IL-34 increased the phosphorylation levels of p38 and mTOR, which could be inhibited by the CSF-1R inhibitor pexidartinib, a p38 inhibitor, or an mTOR inhibitor (Fig. 4C&D). The enhanced macrophage proliferation and migration could also be abolished by these inhibitors, indicating that IL-34 could induce the activation of the p38 and mTOR signaling pathways in macrophages (Fig. 4E&F). |
| Cell Experiment | |
|---|---|
| Cell lines | GIST, MPNST, and ST8814 cells |
| Preparation method | Cell viability assays. Cell viability assays were carried out with the Dojindo Molecular Technologies Kit per manufacturer's instructions. Briefly, 2,000 cells were plated in 96-well plates in RPMI media with 10% FBS and then treated with the indicated drugs the next day. Media were replaced with 100 μL of media with 10% serum and 10% CCK-8 (AbMole) solution. After 1 hour, the optical density was read at 450 nm using a Spectra Max 340 PC (Molecular Devices Corp.) to determine viability. Background values from negative control wells without cells were subtracted for final sample quantification. Data were plotted as % cell viability compared with dimethyl sulfoxide (DMSO; no drug) control. |
| Concentrations | 0~1μM |
| Incubation time | 144h |
| Animal Experiment | |
|---|---|
| Animal models | Ten-week-old mice fed a chow or high-fat diet for 10 weeks |
| Formulation | dissolved in 5% DMSO and 25% PEG300 in ddH2O |
| Dosages | 50 mg/kg every second day for 3 weeks |
| Administration | oral gavage |
| Molecular Weight | 417.81 |
| Formula | C20H15ClF3N5 |
| CAS Number | 1029044-16-3 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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