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Pexidartinib

Cat. No. M4867
Pexidartinib Structure
Synonym:

PLX3397

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 40  USD40 In stock
5mg USD 40  USD40 In stock
10mg USD 55  USD55 In stock
50mg USD 150  USD150 In stock
100mg USD 185  USD185 In stock
500mg USD 390  USD390 In stock
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Quality Control
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
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)
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).
Protocol
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 MPNST xenografts in the flank of ICR/SCID mice
Formulation diet
Dosages 40 mg/kg/day
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 417.81
Formula C20H15ClF3N5
CAS Number 1029044-16-3
Purity 100.0%
Solubility DMSO 15 mg/mL
Storage at -20°C
References

[1] Patwardhan PP, et al. Clin Cancer Res. Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs.

[2] DeNardo DG, et.al. Cancer Discov. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pexidartinib, PLX3397 supplier, c-Kit, inhibitors

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