Pexidartinib (PLX3397)

For research use only. Not for use in humans.

Catalog No.S7818

30 publications

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.

Size Price Stock Quantity  
USD 107 In stock
USD 347 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's Pexidartinib (PLX3397) has been cited by 30 publications

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.
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 NVrMSXVUS2WubDD2bYFjcWyrdImgZZN{[Xl? NYXlPHBNOC5yMT2xNFAhdmdxbVy= MV6yOEBp MYjUdoVifG2nboSge4l1cCCSZYjp[IFzfGmwaXKgLFAvODFvMUCwJI5oN22OKTDmc5IhOjRiaH;1dpMh\GmmIH7veEB{cWewaX\pZ4FvfGy7IHHm[oVkfCCvdYLpcoUhPFRzIHPhdoNqdm:vYTDj[YxtKG63bXLldkBqdiC4aYTyc{BieyCvZXHzeZJm\CCkeTDjdpl{fGGuII\pc4xmfCC|dHHpck4> NV;TeIhKOzB7M{[3N|k>

... Click to View More Cell Line Experimental Data

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]


Animal Research:


- Collapse
  • 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.

* 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


CAS No. 1029044-16-3
Storage powder
in solvent
Synonyms N/A
Smiles FC(F)(F)C1=NC=C(CNC2=NC=C(CC3=C[NH]C4=NC=C(Cl)C=C34)C=C2)C=C1

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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

Tags: buy Pexidartinib (PLX3397) | Pexidartinib (PLX3397) supplier | purchase Pexidartinib (PLX3397) | Pexidartinib (PLX3397) cost | Pexidartinib (PLX3397) manufacturer | order Pexidartinib (PLX3397) | Pexidartinib (PLX3397) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID