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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1 Customer Review

  • (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.

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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]

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:
5% DMSO+45% PEG 300+5% Tween 80+ddH2O
* prepare fresh solution for each experiment
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
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02390752 Recruiting Neurofibroma, Plexiform|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Leukemia, Prolymphocytic, Acute|Sarcoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 6, 2015 Phase 1|Phase 2
NCT02975700 Not yet recruiting Metastatic Melanoma Plexxikon January 2017 Phase 1|Phase 2
NCT02777710 Recruiting Colorectal Cancer|Pancreatic Cancer|Metastatic Cancer|Advanced Cancer Centre Leon Berard|AstraZeneca|Plexxikon June 2016 Phase 1
NCT02734433 Recruiting Advanced Solid Tumors Daiichi Sankyo Co., Ltd.|Quintiles, Inc.|Daiichi Sankyo Inc. June 2016 Phase 1
NCT02071940 Recruiting Malignant Melanoma The Christie NHS Foundation Trust October 2015 Phase 2
NCT02452424 Recruiting Melanoma|Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck|GIST Plexxikon|Merck Sharp & Dohme Corp. June 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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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 10% DMSO/40% PEG 300/ddH2O at 15mg/ml clearly.

Related Antibodies

CSF-1R Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID