Pexidartinib (PLX3397)

Catalog No.S7818

Pexidartinib (PLX3397) Chemical Structure

Molecular Weight(MW): 417.81

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. Phase 3.

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Cited by 16 Publications

6 Customer Reviews

  • (a) Reduced tumour burden in PLX3397 (PLX) treated mice relative to untreated (NT) (n=6, P=.015; unpaired t-test). Bars represent total tumour volume with number of identified tumours indicated above each bar.

    Nat Commun, 2017, 8:14293. Pexidartinib (PLX3397) purchased from Selleck.

  • Quantitative analyses of CSF-1R phosphorylation induced by CSF-1 in macrophages with (open column) and without (solid column) CSF1R c.1085A>G genetic variant. Macrophages differentiated from peripheral blood mononuclear cells were serum starved for 18 hours followed by stimulation with CSF-1 100 ng/mL for 5 minutes with or without pretreatment with CSF-1R inhibitor, PLX3397. The phosphorylation of CSF-1R was measured by phospho-MCSF-receptor sandwich ELISA Kit. Y axis, normalized CSF-1R phosphorylation. Each value represents mean ± SEM from at least seven different samples in each group.

    Clin Cancer Res, 2017, 23(20):6021-6030. Pexidartinib (PLX3397) purchased from Selleck.

  • PLX3397 significantly attenuated the upregulation of CSF1R and CX3CR1 in ipsilateral and contralateral dorsal horn induced by ischemia 6h. Data are presented as mean ± SEM. *P ≤ .05, **P ≤ .01.

    Brain Behav Immun, 2018, 68:248-260. Pexidartinib (PLX3397) purchased from Selleck.

  • C) Immunostaining of CD4+ T cells (CD4, green), CD8+ T cells (CD8, green), B cells (CD19, green), NK cells (NKp46, green), monocytes and macrophages (CD169, green), neutrophils (Ly6G, green), and DAPI (blue).

    FASEB J, 2018, 32(6):3336-3345. Pexidartinib (PLX3397) purchased from Selleck.

  • Microglia contribute to the protective effect of etifoxine. C57BL/6 mice received daily treatment of the colony stimulator factor 1 receptor inhibitor, PLX3397, for 21 days prior to 60 min MCAO. After MCAO and immediately at the onset of reperfusion, mice received a single i.p. injection of etifoxine or vehicle control. At 24 h after MCAO and reperfusion, neurodeficits and infarct volume were determined. a Bar graph shows numbers of CD11b+ CD45int cells in groups of MCAO mice receiving indicated treatments. b Bar graph shows numbers of CD11b+ CD45intTSPO+ cells in groups of MCAO mice receiving indicated treatments. c Bar graph shows numbers of CD11b+CD45high and CD11b−CD45high cells in groups of MCAO mice receiving indicated treatments. d Bar graph shows neurodeficits based on mNSS in MCAO mice receiving indicated treatments. e TTC-stained images show infarct in mice receiving etifoxine or vehicle after MCAO and reperfusion. f Bar graph shows infarct volume in MCAO mice receiving etifoxine or vehicle. n = 8 per group. Data were presented as mean ± SEM.

    J Neuroinflammation, 2017, 14(1):151. Pexidartinib (PLX3397) purchased from Selleck.

  • PLX3397 decreases the BrdU and retinal precursor cell markers, Chx10 or Pax6 (green) double-positive cells.

    Mol Vis, 2018, 30(24):536-545. Pexidartinib (PLX3397) purchased from Selleck.

Purity & Quality Control

Choose Selective CSF-1R Inhibitors

Biological Activity

Description 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. Phase 3.
Targets
Kit [1]
(Cell-free assay)
CSF-1R [1]
(Cell-free assay)
Flt3 [1]
(Cell-free assay)
10 nM 20 nM 160 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
4T1 cells NFfw[GNE\WyuII\pZYJqdGm2eTDhd5NigQ>? MVuwMlAyNTFyMDDu[{9uVA>? NECzTGMzPCCq Mn3PWJJm[XSvZX70JJdqfGhiUHX4bYRienSrbnniJEgxNjBzLUGwNEBv\y:vTDmg[o9zKDJ2IHjveZJ{KGSrZDDuc5Qhe2mpbnnmbYNidnSueTDh[oZm[3RibYXybY5mKDSWMTDjZZJkcW6xbXGgZ4VtdCCwdX3i[ZIhcW5idnn0do8h[XNibXXhd5Vz\WRiYomgZ5J6e3SjbDD2bY9t\XRic4ThbY4v MX2zNFk{Pjd|OR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK; 

PubMed: 24718867     


GIST, MPNST and ST8814 cells were grown to 60% confluency in 60-mm plates and treated for 24 hours with DMSO control or increasing concentrations of PLX3397 (0.5, 1 and 2 μmol/L). 30μg of RIPA lysates were loaded on SDS/PAGE and immunoblotted using indicated antibodies.

p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R; 

PubMed: 28932635     


Shortly after exogenous CSF1 stimulation in RAW264.7 cells, the phosphorylation of CSF1R, MEK1/2, Erk1/2, and c-Jun was increased, which was blocked by PLX3397. The MEK1/2 inhibitor U0126 decreased the phosphorylation of Erk1/2 and c-Jun.

24718867 28932635
In vivo In MMTV-PyMT mice, Pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. [1] In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. [2] In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. [3] In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. [4]

Protocol

Animal Research:

[1]

+ Expand
  • Animal Models: MMTV-PyMT mice
  • Formulation: Formulated in mouse chow
  • Dosages: 40 mg/kg/day
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (198.65 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 417.81
Formula

C20H15ClF3N5

CAS No. 1029044-16-3
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03291288 Active not recruiting Drug: Tolbutamide|Drug: Midazolam|Drug: Pexidartinib Drug Interaction Potential Daiichi Sankyo Inc. February 26 2018 Phase 1
NCT02975700 Active not recruiting Drug: PLX3397 Melanoma Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. January 2017 Not Applicable
NCT02777710 Active not recruiting Drug: Pexidartinib|Drug: Durvalumab Colorectal Cancer|Pancreatic Cancer|Metastatic Cancer|Advanced Cancer Centre Leon Berard|AstraZeneca|Plexxikon June 2016 Phase 1
NCT02071940 Unknown status Drug: PLX3397 Malignant Melanoma The Christie NHS Foundation Trust October 2015 Phase 2
NCT02452424 Terminated Drug: PLX3397|Biological: Pembrolizumab Melanoma|Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck|Gastrointestinal Stromal Tumor (GIST)|Ovarian Cancer Plexxikon|Merck Sharp & Dohme Corp. July 2 2015 Phase 1|Phase 2
NCT02390752 Recruiting Drug: PLX3397 Neurofibroma Plexiform|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Leukemia Prolymphocytic Acute|Sarcoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 29 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I am going to use PLX3397 for mice experiment. but I am not sure how to dissolve it, could you tell me the detail?

  • Answer:

    S7818 Pexidartinib (PLX3397) can dissolve in 5% DMSO+45% PEG 300+5% Tween 80+ddH2O at 10mg/ml.

CSF-1R Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID