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)
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
7.2mg/ml 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. 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 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]
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]

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.

Customer Product Validation

Data from [Data independently produced by , , Nat Commun, 2017, 8:14293]

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

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

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

Selleck's Pexidartinib (PLX3397) has been cited by 107 publications

The aging mouse CNS is protected by an autophagy-dependent microglia population promoted by IL-34 [ Nat Commun, 2024, 15(1):383] PubMed: 38195627
Host-functionalization of macrin nanoparticles to enable drug loading and control tumor-associated macrophage phenotype [ Front Immunol, 2024, 15:1331480] PubMed: 38545103
Microglia-endothelial cross-talk regulates diabetes-induced retinal vascular dysfunction through remodeling inflammatory microenvironment [ iScience, 2024, 27(3):109145] PubMed: 38414848
Colony stimulating factor-1 (CSF-1) signalling is predictive of response to immune checkpoint inhibitors in advanced non-small cell lung cancer [ Lung Cancer, 2024, 188:107447] PubMed: 38176297
Engineering an inhibitor-resistant human CSF1R variant for microglia replacement [ J Exp Med, 2023, 220(3)e20220857] PubMed: 36584406
Polyoxazoline-Based Nanovaccine Synergizes with Tumor-Associated Macrophage Targeting and Anti-PD-1 Immunotherapy against Solid Tumors [ Adv Sci (Weinh), 2023, 10(25):e2300299] PubMed: 37434063
The type-I interferon response potentiates seeded tau aggregation and exacerbates tau pathology [ Alzheimers Dement, 2023, 10.1002/alz.13493] PubMed: 37849026
Repopulated retinal microglia promote Müller glia reprogramming and preserve visual function in retinal degenerative mice [ Theranostics, 2023, 13(5):1698-1715] PubMed: 37056562
Meningeal macrophages inhibit chemokine signaling in pre-tumor cells to suppress mouse medulloblastoma initiation [ Dev Cell, 2023, 10.1038/s41418-023-01234-w] PubMed: 37774709
ZIC2 induces pro-tumor macrophage polarization in nasopharyngeal carcinoma by activating the JUNB/MCSF axis [ Cell Death Dis, 2023, 14(7):455] PubMed: 37479694

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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.