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Pexidartinib (PLX3397)

Name: Pexidartinib (PLX3397)
Brand: Selleck Chemicals
SKU: S7818
Rating: 5 (104 reviews)

Catalog No.S7818 Purity: 99.94%

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

CAS: 1029044-16-3

Selleck's Pexidartinib (PLX3397) has been cited by 104 publications

Purity & Quality Control

Batch: Purity: 99.94%

99.94

Products often used together with Pexidartinib (PLX3397)

Tween 80

Pexidartinib is dissolved in Tween 80 with additional solvents to provide a solution for C57BL/6 mice oral administration of the medication in drinking water.

Ni RJ, et al. Zool Res. 2023;44(3):543-555.

PEG300

Pexidartinib is dissolved in polyethylene glycol 300 (PEG300) with additional solvents to provide a solution for Swiss mice to study the role of microglia in drug abuse.

da Silva MCM, et al. Sci Rep. 2021 Aug 6;11(1):15989.

Rapamycin (Sirolimus)

PLX3397 and Rapamycin combination significantly inhibits tumor growth in malignant peripheral nerve sheath tumor (MPNST) xenografts.

Manji GA, et al. Clin Cancer Res. 2021;27(20):5519-5527.

Imatinib

PLX3397 and Imatinib inhibit malignant peripheral nerve sheath tumor (MPNST) cell proliferation in vitro.

Manji GA, et al. Clin Cancer Res. 2021;27(20):5519-5527.

Dovitinib (TKI-258)

Pexidartinib and Dovitinib combination enhances anti-glioma efficacy in the PDGF-B-driven glioma (PDG) model.

Yan D, et al. Oncogene. 2017;36(43):6049-6058.

Related compound libraries

Choose Selective CSF-1R Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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

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
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
Experimental Result Images	Western blot	p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R		24718867

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04703322	Recruiting	Tenosynovial Giant Cell Tumor	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo Inc.	March 15 2021	Phase 2
NCT04635111	Recruiting	Hepatotoxicity\|Tenosynovial Giant Cell Tumor	Daiichi Sankyo Inc.	January 7 2021	--
NCT04488822	Active not recruiting	Tenosynovial Giant Cell Tumor	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo Inc.	September 25 2020	Phase 3
NCT04223635	Completed	Moderate Hepatic Impairment	Daiichi Sankyo Inc.	January 7 2020	Early Phase 1
NCT03291288	Completed	Drug Interaction Potential	Daiichi Sankyo Inc.	February 26 2018	Phase 1

References

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Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
	Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	7.2mg/ml (17.23mM)	Taking the 1 mL working solution as an example, add 100 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 Corn oil	10.0mg/ml (23.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.65mg/ml (1.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	10.0mg/ml (23.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

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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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