Pexidartinib (PLX3397)

Catalog No.S7818 Batch:S781814

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Technical Data

Formula

C20H15ClF3N5
Molecular Weight 417.81 CAS No. 1029044-16-3
Solubility (25°C)* In vitro DMSO 84 mg/mL (201.04 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 7.200mg/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. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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. This compound induces apoptosis and necrosis with antitumor activity. Phase 3.
Targets
Kit
(Cell-free assay)		 CSF-1R
(Cell-free assay)		 Flt3
(Cell-free assay)
10 nM 20 nM 160 nM
In vitro

In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib (PLX3397) inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μM and 0.1 μM, respectively.

In Vivo

In MMTV-PyMT mice, Pexidartinib (PLX3397) (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumour infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. This compound/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumours, paralleling induction of apoptosis and necrosis.

In C57 mice bearing GL261 tumours, this compound (p.o.) inhibits glioblastoma invasion.

In cmo mice, this chemical significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α.

In mice bearing B16F10 melanomas, this compound (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.

Protocol (from reference)

Kinase Assay:

[1]
  • 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.
Animal Study:

[5]
  • Animal Models

    MMTV-PyMT mice

  • Dosages

    40 mg/kg/day

  • Administration

    p.o.

References

  • https://pubmed.ncbi.nlm.nih.gov/22039576/
  • https://pubmed.ncbi.nlm.nih.gov/22294205/
  • https://pubmed.ncbi.nlm.nih.gov/22923495/
  • https://pubmed.ncbi.nlm.nih.gov/25110953/
  • https://pubmed.ncbi.nlm.nih.gov/35569511/

Customer Product Validation

(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.

Data from [ , , Nat Commun, 2017, 8:14293 ]

Quantitative analyses of CSF-1R phosphorylation induced by CSF-1 in macrophages with (open column) and without (solid column) CSF1R c.1085A>G genetic variant. Macrophages differentiated from peripheral blood mononuclear cells were serum starved for 18 hours followed by stimulation with CSF-1 100 ng/mL for 5 minutes with or without pretreatment with CSF-1R inhibitor, PLX3397. The phosphorylation of CSF-1R was measured by phospho-MCSF-receptor sandwich ELISA Kit. Y axis, normalized CSF-1R phosphorylation. Each value represents mean ± SEM from at least seven different samples in each group.

Data from [ , , Clin Cancer Res, 2017, 23(20):6021-6030 ]

PLX3397 significantly attenuated the upregulation of CSF1R and CX3CR1 in ipsilateral and contralateral dorsal horn induced by ischemia 6h. Data are presented as mean ± SEM. *P ≤ .05, **P ≤ .01.

Data from [ , , Brain Behav Immun, 2018, 68:248-260 ]

C) Immunostaining of CD4+ T cells (CD4, green), CD8+ T cells (CD8, green), B cells (CD19, green), NK cells (NKp46, green), monocytes and macrophages (CD169, green), neutrophils (Ly6G, green), and DAPI (blue).

Data from [ , , FASEB J, 2018, 32(6):3336-3345 ]

Sellecks Pexidartinib (PLX3397) Has Been Cited by 129 Publications

Targeting C1q prevents microglia-mediated synaptic removal in neuropathic pain [ Nat Commun, 2025, 16(1):4590] PubMed: 40382320
Small intestinal γδ T17 cells promote SAE through STING/C1q-induced microglial synaptic pruning in male mice [ Nat Commun, 2025, 16(1):6779] PubMed: 40702081
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells [ Mol Ther, 2025, S1525-0016(25)00871-8] PubMed: 41232525
Stress induces behavioral disorders by promoting microglial phagocytosis via decreasing neuronal Dkk3 [ Mol Psychiatry, 2025, 30(12):5731-5748] PubMed: 41136744
Exosome-mediated microglia-astrocyte interactions drive neuroinflammation in Parkinson's disease with Peli1 as a potential therapeutic target [ Pharmacol Res, 2025, 219:107908] PubMed: 40816423
Deciphering the preeclampsia-specific immune microenvironment and the role of pro-inflammatory macrophages at the maternal-fetal interface [ Elife, 2025, 13RP100002] PubMed: 40152904
Depletion of HSP60 in Microglia Leads to Synaptic Dysfunction and Depression-Like Behaviors Through Enhanced Synaptic Pruning in Male Mice [ CNS Neurosci Ther, 2025, 31(4):e70394] PubMed: 40237297
C3/C3aR Bridges Spinal Astrocyte-Microglia Crosstalk and Accelerates Neuroinflammation in Morphine-Tolerant Rats [ CNS Neurosci Ther, 2025, 31(1):e70216] PubMed: 39801259
Macrophage polarization, inflammatory monocytes, and impaired MDSCs are associated with murine and human immune aplastic anemia [ J Leukoc Biol, 2025, 117(6)qiaf073] PubMed: 40411822
Mechanistic study of pexidartinib-induced toxicity in human hepatic cells [ Chem Biol Interact, 2025, 419:111641] PubMed: 40617559

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.