Pexidartinib hydrochloride
Based on 161 publication(s) in Google Scholar
Pexidartinib hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 2040295-03-0
- Formula: C20H16Cl2F3N5
- Molecular Weight:454.28
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Pexidartinib hydrochloride
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- Nature. 2022 Mar;603(7899):138-144. [Abstract]
- Science. 2026 May 21;392(6800):eaeb6999. [Abstract]
- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Cell. 2026 Jan 22:S1535-6108(25)00554-9. [Abstract]
- Cancer Cell. 2023 Nov 13;41(11):1911-1926.e8. [Abstract]
- Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]
- Cell Metab. 2026 Jun 4:S1550-4131(26)00191-9. [Abstract]
- Nat Immunol. 2023 May;24(5):827-840. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Nat Metab. 2024 Aug;6(8):1479-1491. [Abstract]
- Cell Stem Cell. 2025 Apr 9:S1934-5909(25)00099-2. [Abstract]
- Cell Stem Cell. 2025 Jan 2;32(1):86-104.e7. [Abstract]
- Nat Neurosci. 2025 Jul;28(7):1404-1417. [Abstract]
- Circ Res. 2021 Sep 17;129(7):e121-e140. [Abstract]
- ACS Nano. 2024 Jan 30;18(4):3295-3312. [Abstract]
- Nat Commun. 2024 Oct 13;15(1):8837. [Abstract]
- Nat Commun. 2024 Jul 5;15(1):5654. [Abstract]
- Neuron. 2026 Mar 26:S0896-6273(26)00128-5. [Abstract]
- Neuron. 2021 Aug 18;109(16):2573-2589.e9. [Abstract]
- Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]
- Adv Sci (Weinh). 2024 Dec 12:e2413451. [Abstract]
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- Interdiscip Med. 2025 Feb 24.
- Theranostics. 2020 Jan 1;10(1):74-90. [Abstract]
- Mol Ther. 2025 Nov 12:S1525-0016(25)00871-8. [Abstract]
- Mol Ther. 2025 Nov 12:S1525-0016(25)00872-X. [Abstract]
- Alzheimers Dement. 2026 Jun;22(6):e71579. [Abstract]
- Nat Cardiovasc Res. 2023 Jun;2(6):572-586. [Abstract]
- Cell Rep Med. 2026 Jun 16;7(6):102833. [Abstract]
- J Immunother Cancer. 2025 Jul 15;13(7):e010926. [Abstract]
- Cell Rep Med. 2025 Jun 23:102204. [Abstract]
- J Exp Med. 2023 Mar 6;220(3):e20220857. [Abstract]
- Pharmacol Res. 2023 May:191:106773. [Abstract]
- J Neuroinflammation. 2026 May 26. [Abstract]
- Int J Surg. 2026 Apr.
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- J Neuroinflammation. 2024 Sep 1;21(1):215. [Abstract]
- J Neuroinflammation. 2023 Feb 25;20(1):51. [Abstract]
- Cancer Lett. 2022 Sep 1:543:215795. [Abstract]
- J Neuroinflammation. 2022 Jan 21;19(1):20. [Abstract]
- J Neuroinflammation. 2020 Jan 23;17(1):31. [Abstract]
- Cell Death Dis. 2025 Dec 10. [Abstract]
- Dev Cell. 2025 Apr 21;60(8):1199-1216.e7. [Abstract]
- Phytomedicine. 2025 Nov 29:150:157636. [Abstract]
- EMBO Mol Med. 2024 Dec;16(12):3113-3141. [Abstract]
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- Diabetes. 2023 Nov 1;72(11):1692-1706. [Abstract]
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- Neurotherapeutics. 2025 Dec 11:e00818. [Abstract]
- Cell Rep. 2024 Oct 23;43(11):114894. [Abstract]
- Cell Rep. 2023 Sep 22;42(10):113128. [Abstract]
- Neural Regen Res. 2023 Sep;18(9):2067-2074. [Abstract]
- Inflamm Regen. 2024 Jun 6;44(1):30. [Abstract]
- Transl Psychiatry. 2025 Aug 15;15(1):285. [Abstract]
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- Transl Psychiatry. 2020 Jan 27;10(1):32. [Abstract]
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- Front Immunol. 2022 May 13;13:866073. [Abstract]
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- J Am Heart Assoc. 2023 Jun 20;12(12):e029053. [Abstract]
- Cells. 2021 Jul 22;10(8):1862. [Abstract]
- Cells. 2021 Apr 12;10(4):874. [Abstract]
- Cancer Immunol Immunother. 2026 Apr 6;75(5):137. [Abstract]
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- Glia. 2022 Nov;70(11):2032-2044. [Abstract]
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- CNS Neurosci Ther. 2023 Jun;29 Suppl 1(Suppl 1):146-160. [Abstract]
- Int J Mol Sci. 2024 Jun 26;25(13):7001. [Abstract]
- Biomolecules. 2022 May 4;12(5):666. [Abstract]
- Cell Oncol (Dordr). 2021 Feb;44(1):193-204. [Abstract]
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- Invest Ophthalmol Vis Sci. 2025 Mar 3;66(3):4. [Abstract]
- Int Immunopharmacol. 2025 Apr 16:152:114428. [Abstract]
- Int Immunopharmacol. 2023 May:118:109976. [Abstract]
- Am J Physiol Cell Physiol. 2020 Sep 1;319(3):C605-C610. [Abstract]
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- Neuropharmacology. 2020 Aug 1;172:108132. [Abstract]
- Neuropharmacology. 2019 Jun:151:33-44. [Abstract]
- Transl Stroke Res. 2025 Aug;16(4):1075-1093. [Abstract]
- iScience. 2026 Jan 7;29(2):114638. [Abstract]
- J Neurosci. 2020 May 6;40(19):3862-3879. [Abstract]
- Sci Rep. 2024 Aug 4;14(1):18031. [Abstract]
- Biomedicines. 2022 Jul 9;10(7):1653. [Abstract]
- Biomedicines. 2021 Oct 4;9(10):1387. [Abstract]
- Sci Rep. 2021 Aug 6;11(1):15989. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jul 13;101:109931. [Abstract]
- Int Dent J. 2025 Jun 2;75(4):100843. [Abstract]
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- Endocrinology. 2024 Feb 20;165(4):bqae003. [Abstract]
- J Neurooncol. 2021 Jun;153(2):225-237. [Abstract]
- Mol Pharmacol. 2022 Jun;101(6):381-389. [Abstract]
- Life Sci Alliance. 2023 Aug 7;6(11):e202302020. [Abstract]
- Immunol Lett. 2026 Apr 27:107179. [Abstract]
- J Mol Neurosci. 2025 Aug 2;75(3):97. [Abstract]
- Brain Behav. 2025 Mar;15(3):e70369. [Abstract]
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- Brain Res. 2026 Aug 15:1885:150332. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- J Ocul Pharmacol Ther. 2020 Jun;36(5):311-319. [Abstract]
- J Anat. 2023 Sep;243(3):394-403. [Abstract]
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- STAR Protoc. 2023 Jul 29;4(3):102490. [Abstract]
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- Albert Einstein College of Medicine. 2026.
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- University of Washington. 2025.
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- bioRxiv. 2025 Jul 17:2025.07.12.664223. [Abstract]
- University of Cambridge. 2025
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- Res Sq. 2025 Feb 10.
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- bioRxiv. 2024 Jun 6:2024.06.05.597614. [Abstract]
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- Research Square Preprint. 2024 Feb 15.
- bioRxiv. 2023 Nov 17:2023.11.16.567274. [Abstract]
- bioRxiv. 2023 Nov 14:2023.11.10.566510. [Abstract]
- The Ohio State University. 2023 Oct.
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- Res Sq. 2023 Sep 12:rs.3.rs-3263412. [Abstract]
- Universität zu Köln. 2023 Sep 26.
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- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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WB
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In Vivo Efficacy Study
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In Vivo Imaging
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IF
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In Vivo Efficacy Study
Biological Activity
IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1]
Pexidartinib hydrochloride (PLX-3397 hydrochloride) 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.
Pexidartinib (290 ppm in AIN-76A standard chow, 21 days) hydrochloride 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 ) hydrochloride depletes the microglia cells more than 90% in brain of C57BL/6J mice[6].
Pexidartinib hydrochloride (0.25, 1 mg/kg, i.p., twice daily for 8 days) hydrochloride inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2].
Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) hydrochloride shows no obvious effect on the cleaved caspase-3-positive cells in mice[2].
Pexidartinib hydrochloride (50 mg/kg; p.o.; every second day for 3 weeks) hydrochloride reduces tissue macrophage levels without affecting glucose homeostasis in mice[4].
Pexidartinib hydrochloride has limited permeability to the blood-brain barrier, primarily through ABCB1[7].
Pexidartinib hydrochloride can mainly penetrate the damaged blood-brain barrier surrounding the tumor, allowing tumor cells to enter the intact blood-brain barrier[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neonatal mice[2]
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Dosage:0.25, 1 mg/kg
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Administration:I.P. twice daily for 8 days
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Result:Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells.
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Animal Model:10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice)[4]
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Dosage:50 mg/kg
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Administration:P.o.; every second day for 3 weeks
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Result:Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels.
Chemical Information
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CAS No. 2040295-03-0
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Appearance Solid
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Molecular Weight 454.28
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Formula C20H16Cl2F3N5
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Color White to off-white
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SMILES
FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F.Cl
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Synonyms
PLX-3397 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (161)
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Journal Impact Factor
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Most Recent
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Nature
2024 Apr;628(8006):145-153. PMID: 38538785 -
Nature
2022 Mar;603(7899):138-144. PMID: 35197636 -
Science
Microglia Rank signaling regulates GnRH neuronal function and the hypothalamic-pituitary-gonadal axis. [Abstract]2026 May 21;392(6800):eaeb6999. PMID: 41818388 -
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Cancer Cell
IGSF11-VISTA is a critical and targetable immune checkpoint axis in diffuse midline glioma. [Abstract]2026 Jan 22:S1535-6108(25)00554-9. PMID: 41576930 -
Cancer Cell
TIM-3 blockade in diffuse intrinsic pontine glioma models promotes tumor regression and antitumor immune memory. [Abstract]2023 Nov 13;41(11):1911-1926.e8. PMID: 37802053
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Nov 13;41(11):1911-1926.e8. [Abstract]
PLX-3397 was administered orally at 50 mg/kg every day beginning on the day before the first antibody administration.
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Cancer Cell
2021 Oct 11;39(10):1361-1374.e9. PMID: 34478639 -
Cell Metab
2026 Jun 4:S1550-4131(26)00191-9. PMID: 42242219 -
Nat Immunol
MafB-restricted local monocyte proliferation precedes lung interstitial macrophage differentiation. [Abstract]2023 May;24(5):827-840. PMID: 36928411
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 May;24(5):827-840. [Abstract]
100 mg per kg body weight of pexidartinib was injected i.p. 24 and 48 h after DT injection. Representative histograms of EdU levels in lung extravascular CD64+ cells from DT-treated IMDTR mice that were treated with DT i.p. 3 days before, with the Csf1r antagonist PLX-3397 or with vehicle i.p. 1 and 2 days before, and with EdU i.p. 8 h before.
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Nat Metab
Microglia mitochondrial complex I deficiency during development induces glial dysfunction and early lethality. [Abstract]2024 Aug;6(8):1479-1491. PMID: 39048800 -
Cell Stem Cell
2025 Apr 9:S1934-5909(25)00099-2. PMID: 40233761 -
Cell Stem Cell
Microglia depletion reduces human neuronal APOE4-related pathologies in a chimeric Alzheimer's disease model. [Abstract]2025 Jan 2;32(1):86-104.e7. PMID: 39500314
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2025 Jan 2;32(1):86-104.e7. [Abstract]
PLX3397 was incorporated into AIN-76A chow at a concentration of 400 mg/kg. Chimeric mice were fed either a control AIN-76A chow for 8 months, or fed control AIN-76A chow for 4 months and then PLX chow for 4 months. Representative images of microglia (Iba1, red) in the hippocampus of chimeric mice of each condition were shown. Scale bar, 500 μm.
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Nat Neurosci
GABA-dependent microglial elimination of inhibitory synapses underlies neuronal hyperexcitability in epilepsy. [Abstract]2025 Jul;28(7):1404-1417. PMID: 40425792 -
Circ Res
2021 Sep 17;129(7):e121-e140. PMID: 34399581 -
ACS Nano
Tumor-Microenvironment-Activatable Nanoparticle Mediating Immunogene Therapy and M2 Macrophage-Targeted Inhibitor for Synergistic Cancer Immunotherapy. [Abstract]2024 Jan 30;18(4):3295-3312. PMID: 38252684 -
Nat Commun
In vivo imaging in mouse spinal cord reveals that microglia prevent degeneration of injured axons. [Abstract]2024 Oct 13;15(1):8837. PMID: 39397028 -
Nat Commun
CNS-wide repopulation by hematopoietic-derived microglia-like cells corrects progranulin deficiency in mice. [Abstract]2024 Jul 5;15(1):5654. PMID: 38969669 -
Neuron
Microglia-mediated protection against Alzheimer's disease pathology and detrimental effects in white matter revealed by Ptpn6 deletion. [Abstract]2026 Mar 26:S0896-6273(26)00128-5. PMID: 41895269 -
Neuron
Early-life inflammation promotes depressive symptoms in adolescence via microglial engulfment of dendritic spines. [Abstract]2021 Aug 18;109(16):2573-2589.e9. PMID: 34233151 -
Autophagy
Kit-mediated autophagy suppression driven by a viral oncoprotein emerges as a crucial survival mechanism in Merkel cell carcinoma. [Abstract]2025 Jul;21(7):1523-1543. PMID: 40108758
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Jul;21(7):1523-1543. [Abstract]
Pexidartinib hydrochloride (0.01, 0.05, 0.1, 0.5, 1, 5, 10, 20 μM; 24 h) decreased the expression of p-Y719-KIT and increased the expression of cleaved PARP1 in a dose-dependent manner in WaGa cells.
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Adv Sci (Weinh)
Microglia Process α-Synuclein Fibrils and Enhance their Pathogenicity in a TREM2-Dependent Manner. [Abstract]2024 Dec 12:e2413451. PMID: 39665233 -
Adv Sci (Weinh)
Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]2024 Dec 5:e2410360. PMID: 39639496 -
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Theranostics
Microglia exacerbate white matter injury via complement C3/C3aR pathway after hypoperfusion. [Abstract]2020 Jan 1;10(1):74-90. PMID: 31903107 -
Mol Ther
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells. [Abstract]2025 Nov 12:S1525-0016(25)00871-8. PMID: 41232525 -
Mol Ther
2025 Nov 12:S1525-0016(25)00872-X. PMID: 41232524 -
Alzheimers Dement
2026 Jun;22(6):e71579. PMID: 42252510 -
Nat Cardiovasc Res
Blockade of IL-6 signaling alleviates atherosclerosis in Tet2-deficient clonal hematopoiesis. [Abstract]2023 Jun;2(6):572-586. PMID: 37539077 -
Cell Rep Med
Fungal metabolite-based immunotherapy overcomes tumor-associated macrophage immunosuppression. [Abstract]2026 Jun 16;7(6):102833. PMID: 42173096 -
J Immunother Cancer
Anti-galectin-9 therapy synergizes with EGFR inhibition to reprogram the tumor microenvironment and overcome immune evasion. [Abstract]2025 Jul 15;13(7):e010926. PMID: 40664443 -
Cell Rep Med
Targeting the CD40 costimulatory receptor to improve virotherapy efficacy in diffuse midline gliomas. [Abstract]2025 Jun 23:102204. PMID: 40578365 -
J Exp Med
2023 Mar 6;220(3):e20220857. PMID: 36584406 -
Pharmacol Res
Proinflammatory activation of microglia in the cerebellum hyperexcites Purkinje cells to trigger ataxia. [Abstract]2023 May:191:106773. PMID: 37068531 -
J Neuroinflammation
2026 May 26. PMID: 42185903 -
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J Neuroinflammation
Dihydroartemisinin enhances remyelination by switching microglia to the reparative phenotype. [Abstract]2025 Aug 1;22(1):197. PMID: 40750890 -
J Neuroinflammation
2025 Mar 5;22(1):67. PMID: 40045320 -
J Neuroinflammation
Prolactin deficiency drives diabetes-associated cognitive dysfunction by inducing microglia-mediated synaptic loss. [Abstract]2024 Nov 14;21(1):295. PMID: 39543619 -
J Neuroinflammation
Microglia ameliorate delirium-like phenotypes in a murine model of acute ventilator-induced lung injury. [Abstract]2024 Oct 21;21(1):270. PMID: 39434161 -
J Neuroinflammation
Microglia either promote or restrain TRAIL-mediated excitotoxicity caused by Aβ1-42 oligomers. [Abstract]2024 Sep 1;21(1):215. PMID: 39218898 -
J Neuroinflammation
2023 Feb 25;20(1):51. PMID: 36841828
Pexidartinib hydrochloride 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.
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Cancer Lett
Dual inhibition of TGFβ signaling and CSF1/CSF1R reprograms tumor-infiltrating macrophages and improves response to chemotherapy via suppressing PD-L1. [Abstract]2022 Sep 1:543:215795. PMID: 35718267 -
J Neuroinflammation
An overlooked subset of Cx3cr1wt/wt microglia in the Cx3cr1CreER-Eyfp/wt mouse has a repopulation advantage over Cx3cr1CreER-Eyfp/wt microglia following microglial depletion. [Abstract]2022 Jan 21;19(1):20. PMID: 35062962 -
J Neuroinflammation
Neuroprotective effect of microglia against impairments of auditory steady-state response induced by anti-P IgG from SLE patients in naïve mice. [Abstract]2020 Jan 23;17(1):31. PMID: 31973738
Pexidartinib hydrochloride 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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Cell Death Dis
Identification and targeting oxidative phosphorylation/glycolysis to overcome anti-CSF-1R therapy resistance in glioblastoma. [Abstract]2025 Dec 10. PMID: 41365876 -
Dev Cell
Latent epigenetic programs in Müller glia contribute to stress and disease response in the retina. [Abstract]2025 Apr 21;60(8):1199-1216.e7. PMID: 39753128 -
Phytomedicine
Rapid antiepileptic activity identification of isopimpinellin using a multi-model of epilepsy based on behavior-biomarker-BBB screening pipeline. [Abstract]2025 Nov 29:150:157636. PMID: 41351986 -
EMBO Mol Med
APOE from astrocytes restores Alzheimer's Aβ-pathology and DAM-like responses in APOE deficient microglia. [Abstract]2024 Dec;16(12):3113-3141. PMID: 39528861 -
BMC Med
CSF1R regulates schizophrenia-related stress response and vascular association of microglia/macrophages. [Abstract]2023 Aug 4;21(1):286. PMID: 37542262 -
Brain Behav Immun
IL-17A-mediated copper accumulation participates in chronic neuropathic pain-induced cognitive impairment by enhancing microglial synaptic pruning. [Abstract]2025 Dec 3:132:106208. PMID: 41349925 -
Brain Behav Immun
Microglial homeostasis disruption modulates non-rapid eye movement sleep duration and neuronal activity in adult female mice. [Abstract]2023 Jan:107:153-164. PMID: 36202169 -
Diabetes
2023 Nov 1;72(11):1692-1706. PMID: 37683051 -
Aging Cell
DP1 Receptor Blockade Attenuates Microglial Senescence and Cognitive Decline Caused by PTGDS in Exosomes From Aged Brains. [Abstract]2025 Sep 19:e70228. PMID: 40974022 -
Neurotherapeutics
Sunitinib attenuates secondary injury via the regulation of peri-hematomal microglia at the acute phase of intracerebral hemorrhage. [Abstract]2025 Dec 11:e00818. PMID: 41387160 -
Cell Rep
2024 Oct 23;43(11):114894. PMID: 39446583 -
Cell Rep
Pannexin-1 opening in neuronal edema causes cell death but also leads to protection via increased microglia contacts. [Abstract]2023 Sep 22;42(10):113128. PMID: 37742194 -
Neural Regen Res
Suppressing high mobility group box-1 release alleviates morphine tolerance via the adenosine 5'-monophosphate-activated protein kinase/heme oxygenase-1 pathway. [Abstract]2023 Sep;18(9):2067-2074. PMID: 36926733 -
Inflamm Regen
CX3CL1-CX3CR1 axis protects retinal ganglion cells by inhibiting microglia activation in a distal optic nerve trauma model. [Abstract]2024 Jun 6;44(1):30. PMID: 38844990 -
Transl Psychiatry
Microglia-mediated inflammation and synaptic pruning contribute to sleep deprivation-induced mania in a sex-specific manner. [Abstract]2025 Aug 15;15(1):285. PMID: 40817224 -
Transl Psychiatry
Switch to phagocytic microglia by CSFR1 inhibition drives amyloid-beta clearance from glutamatergic terminals rescuing LTP in acute hippocampal slices. [Abstract]2024 Aug 23;14(1):338. PMID: 39179543 -
Transl Psychiatry
Essential role of microglial transforming growth factor-β1 in antidepressant actions of (R)-ketamine and the novel antidepressant TGF-β1. [Abstract]2020 Jan 27;10(1):32. PMID: 32066676 -
JCI Insight
Immunomodulation of inflammatory responses preserves retinal integrity in murine models of pericyte-depletion retinopathy. [Abstract]2025 Jul 1;10(15):e184465. PMID: 40591415
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Jul 1;10(15):e184465. [Abstract]
PLX3397 groups were fed a diet containing Pexidartinib hydrochloride (PLX3397; 1,200 ppm) for 7 days starting at weaning (p21) and maintained for 7 days before analysis at 4-weeks of age (P28). (A&B) Representative images of retina cryo-sections stained for Iba1 and GFAP, respectively. (C) Representative merged images of CD31 and Iba1 staining of retina whole mounts in IgG and APB5-treated mice with or without administration of PLX3397.
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: JCI Insight. 2025 Jul 1;10(15):e184465. [Abstract]
PLX3397 groups were fed a diet containing Pexidartinib hydrochloride (PLX3397; 1,200 ppm) for 7 days starting at weaning (p21) and maintained for 7 days before analysis at 4-weeks of age (P28). Fluorescein angiographic images.
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Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]
PLX-3397 decreases Iba-1 expression, but has no impact on GFAP expression, in primary cultures of astrocytes. (A) Representative immunoblots of GFAP, Iba-1 and GAPDH with no exposure (−) and exposure to 0.2 µm, 1 µm and 5 µM Pexidartinib hydrochloride (PLX-3397; 17 days). Densitometric analysis of (B) Iba-1 and (C) GFAP was performed with ImageJ software using GAPDH as loading control.
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]
Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 17 days) decreased the percentage of Iba-1-expressing cells in primary cultures of astrocytes.
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]
Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 10, 17 days) did not compromise the viability of cultured astrocytes.
Pexidartinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 May 4;12(5):666. [Abstract]
Pexidartinib hydrochloride (PLX-3397; 0.2, 1, 5 μM; 17 days) decreases the reactivity of cultured astrocytes. (A) Representative immunoblots of C3, PTX3 and GAPDH with no exposure (−) and exposure to 0.2 µm, 1 µm and 5 µM of PLX-3397. Densitometric analysis of (B) C3 and (C) PTX3 was performed with ImageJ software using GAPDH as loading control.
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Inhibition of CSF1R, a receptor involved in microglia viability, alters behavioral and molecular changes induced by cocaine. [Abstract]2021 Aug 6;11(1):15989. PMID: 34362959 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvent & Solubility
DMSO : 60 mg/mL (132.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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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
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2013 mL | 11.0064 mL | 22.0129 mL | 55.0321 mL |
| 5 mM | 0.4403 mL | 2.2013 mL | 4.4026 mL | 11.0064 mL | |
| 10 mM | 0.2201 mL | 1.1006 mL | 2.2013 mL | 5.5032 mL | |
| 15 mM | 0.1468 mL | 0.7338 mL | 1.4675 mL | 3.6688 mL | |
| 20 mM | 0.1101 mL | 0.5503 mL | 1.1006 mL | 2.7516 mL | |
| 25 mM | 0.0881 mL | 0.4403 mL | 0.8805 mL | 2.2013 mL | |
| 30 mM | 0.0734 mL | 0.3669 mL | 0.7338 mL | 1.8344 mL | |
| 40 mM | 0.0550 mL | 0.2752 mL | 0.5503 mL | 1.3758 mL | |
| 50 mM | 0.0440 mL | 0.2201 mL | 0.4403 mL | 1.1006 mL | |
| 60 mM | 0.0367 mL | 0.1834 mL | 0.3669 mL | 0.9172 mL | |
| 80 mM | 0.0275 mL | 0.1376 mL | 0.2752 mL | 0.6879 mL | |
| 100 mM | 0.0220 mL | 0.1101 mL | 0.2201 mL | 0.5503 mL |