Pexidartinib (Synonyms: PLX-3397)

Name: Pexidartinib
Brand: MedChemExpress
SKU: HY-16749
Rating: 5.0 (90 reviews)

Cat. No.: HY-16749 Purity: 99.17%: FAQs
Data Sheet SDS COA Handling Instructions

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Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC₅₀s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.

For research use only. We do not sell to patients.

Pexidartinib Chemical Structure

CAS No. : 1029044-16-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
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5 g	USD 2650	In-stock	Estimated Time of Arrival: December 31
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Based on 90 publication(s) in Google Scholar

Other Forms of Pexidartinib:

Pexidartinib hydrochloride In-stock

88 Publications Citing Use of MCE Pexidartinib

: Pexidartinib purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Feb 25;20(1):51. [Abstract]; Pexidartinib (PLX3397; 290 mg/kg; in animal feedings; for 3 weeks) significantly decreases Iba-1 immunoreactive area in the mouse brains.

: Pexidartinib purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2020 Jan 23;17(1):31. [Abstract]; Representative Iba-1 immunofluorescent staining from the cortex and hippocampus in control and PLX3397-treated mice.

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Biological Activity
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References
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Description

IC₅₀ & Target

IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	EC₅₀	200 nM Compound: 1	Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method	[PMID: 34606263]
BMDM	IC₅₀	> 10 μM Compound: 1	Growth inhibition of CSF2-induced mouse BMDM cell assessed as inhibition of M1 like macrophage growth for 3 days by WST-8 assay Growth inhibition of CSF2-induced mouse BMDM cell assessed as inhibition of M1 like macrophage growth for 3 days by WST-8 assay	[PMID: 34606263]
BMDM	IC₅₀	0.056 μM Compound: 1	Growth inhibition of CSF1-induced mouse BMDM cell assessed as inhibition of M2 like macrophage growth incubated for 3 days by WST-8 assay Growth inhibition of CSF1-induced mouse BMDM cell assessed as inhibition of M2 like macrophage growth incubated for 3 days by WST-8 assay	[PMID: 34606263]
Caco-2	CC₅₀	41.53 μM Compound: PEXIDARTINIB	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	5.43 μM Compound: PEXIDARTINIB	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
NFS-60	EC₅₀	294 nM Compound: 1	Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method	[PMID: 34606263]
NFS-60	IC₅₀	33 nM Compound: Pexidartinib	Antiproliferative activity against CSF1-treated mouse NFS-60 cells measured after 72 hrs by resazurin method Antiproliferative activity against CSF1-treated mouse NFS-60 cells measured after 72 hrs by resazurin method	[PMID: 35961461]
NFS-60	IC₅₀	33 nM Compound: 1	Antiproliferative activity against CSF1-treated mouse NFS-60 cells measured after 72 hrs by resazurin method Antiproliferative activity against CSF1-treated mouse NFS-60 cells measured after 72 hrs by resazurin method	[PMID: 35961460]
RAW264.7	CC₅₀	20.52 μM Compound: 1; PLX3397	Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay	[PMID: 31934767]
RAW264.7	IC₅₀	400 nM Compound: 1; PLX3397	Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha release measured after 24 hrs by ELISA Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha release measured after 24 hrs by ELISA	[PMID: 31934767]
RAW264.7	IC₅₀	430 nM Compound: 1; PLX3397	Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 release measured after 24 hrs by ELISA Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 release measured after 24 hrs by ELISA	[PMID: 31934767]
RBL-2H3	IC₅₀	> 1000 nM Compound: PLX-3397	Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells assessed as induction of degranulation by measuring beta-hexosaminidase release using P-nitrophenyl-N-acetyl-D-glucosamide as substrate measured after 1 hr by microplate reader Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells assessed as induction of degranulation by measuring beta-hexosaminidase release using P-nitrophenyl-N-acetyl-D-glucosamide as substrate measured after 1 hr by microplate reader	[PMID: 34476950]

In Vitro

Pexidartinib (PLX-3397) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC₅₀s of 160, 350, 860, 880, and 890 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pexidartinib can be used to deplete the microglia cells in mice.
Pexidartinib (290 ppm in AIN-76A standard chow, 21 days) depletes the microglia cells in brain by 70% in adult male C57BL/6?J mice (20–25?g)^[5].
Pexidartinib (600 ppm in chow, 10 days and 30 days ) depletes the microglia cells more than 90% in brain of C57BL/6J mice^[6].
Pexidartinib (PLX3397; 0.25, 1 mg/kg, twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice^[2].
Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice^[2].
Pexidartinib (50?mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Neonatal mice^[2]
Dosage:	0.25, 1 mg/kg
Administration:	I.P. twice daily for 8 days
Result:	Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells.

Animal Model:	10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice)^[4]
Dosage:	50 mg/kg
Administration:	P.o.; every second day for 3 weeks
Result:	Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels.

Clinical Trial

Molecular Weight

417.81

Formula

C₂₀H₁₅ClF₃N₅

CAS No.

1029044-16-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (239.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3934 mL	11.9672 mL	23.9343 mL
5 mM	0.4787 mL	2.3934 mL	4.7869 mL
10 mM	0.2393 mL	1.1967 mL	2.3934 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 5 mg/mL (11.97 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (23.93 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.64%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (246 KB) HNMR (249 KB) RP-HPLC (232 KB) MS (58 KB) Elemental Analysis Report (104 KB)

Handling Instructions (2659 KB)

References

[1]. DeNardo DG, et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67. [Content Brief]

[2]. Kuse Y, et al. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018. [Content Brief]

[3]. Lee JH, et al. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2. [Content Brief]

[4]. Merry TL, et al. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2020;44(1):245-253. [Content Brief]

[5]. Luo L, et al. Intermittent theta-burst stimulation improves motor function by inhibiting neuronal pyroptosis and regulating microglial polarization via TLR4/NFκB/NLRP3 signaling pathway in cerebral ischemic mice. J Neuroinflammation. 2022 Jun 11;19(1):141. [Content Brief]

[6]. Chadarevian JP, et al. Engineering an inhibitor-resistant human CSF1R variant for microglia replacement. J Exp Med. 2023 Mar 6;220(3):e20220857. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3934 mL	11.9672 mL	23.9343 mL	59.8358 mL
	5 mM	0.4787 mL	2.3934 mL	4.7869 mL	11.9672 mL
	10 mM	0.2393 mL	1.1967 mL	2.3934 mL	5.9836 mL
	15 mM	0.1596 mL	0.7978 mL	1.5956 mL	3.9891 mL
	20 mM	0.1197 mL	0.5984 mL	1.1967 mL	2.9918 mL
	25 mM	0.0957 mL	0.4787 mL	0.9574 mL	2.3934 mL
	30 mM	0.0798 mL	0.3989 mL	0.7978 mL	1.9945 mL
	40 mM	0.0598 mL	0.2992 mL	0.5984 mL	1.4959 mL
	50 mM	0.0479 mL	0.2393 mL	0.4787 mL	1.1967 mL
	60 mM	0.0399 mL	0.1995 mL	0.3989 mL	0.9973 mL
	80 mM	0.0299 mL	0.1496 mL	0.2992 mL	0.7479 mL
	100 mM	0.0239 mL	0.1197 mL	0.2393 mL	0.5984 mL

Pexidartinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pexidartinib1029044-16-3PLX-3397PLX3397PLX 3397c-Fmsc-KitApoptosisCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RSCFRCD117Inhibitorinhibitorinhibit

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Pexidartinib (Synonyms: PLX-3397)

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Other Forms of Pexidartinib:

Pexidartinib Related Antibodies

88 Publications Citing Use of MCE Pexidartinib

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Pexidartinib Related Antibodies

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Complete Stock Solution Preparation Table

Pexidartinib Related Classifications

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