Pexidartinib (PLX3397)

Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.

Pexidartinib (PLX3397) Chemical Structure

Pexidartinib (PLX3397) Chemical Structure

CAS No. 1029044-16-3

Purity & Quality Control

Pexidartinib (PLX3397) Related Products

Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
4T1 cells Cell viability assay 0.01-100 ng/mL 24 h Treatment with Pexidartinib (0.01-100 ng/mL) for 24 hours did not significantly affect murine 4T1 carcinoma cell number in vitro as measured by crystal violet stain. 30936739
Caco-2 cells Cytotoxicity assay 48 h IC50 = 5.43 μM ChEMBL
Caco-2 cells Cell Viability Assay 48 h CC50 = 41.53 μM ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. 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 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]

Kinase Assay Kinase assay
PLX3397 is identified as a potent CSF-1R and c-KIT kinase inhibitor by using a Scaffold- and X-ray structure-based discovery approach. The IC50 data are from SelectScreen™ profiling service.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK 28932635
In Vivo
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 Animal Models MMTV-PyMT mice
Dosages 40 mg/kg/day
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04703322 Recruiting
Tenosynovial Giant Cell Tumor
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo
March 15 2021 Phase 2
NCT04635111 Recruiting
Hepatotoxicity|Tenosynovial Giant Cell Tumor
Daiichi Sankyo
January 7 2021 --
NCT04488822 Active not recruiting
Tenosynovial Giant Cell Tumor
Daiichi Sankyo Co. Ltd.|Daiichi Sankyo
September 25 2020 Phase 3
NCT04223635 Completed
Moderate Hepatic Impairment
Daiichi Sankyo
January 7 2020 Early Phase 1
NCT03291288 Completed
Drug Interaction Potential
Daiichi Sankyo
February 26 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 417.81 Formula

C20H15ClF3N5

CAS No. 1029044-16-3 SDF Download Pexidartinib (PLX3397) SDF
Smiles C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (201.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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

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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.

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