| Field | Specification |
|---|---|
| Alternative names | PLX-3397 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H15ClF3N5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Pexidartinib, also known as PLX-3397, is a potent, orally active, selective and ATP-competitive inhibitor of colony stimulating factor 1 receptor (CSF1R, also called M-CSFR) and c-Kit, with IC50 values of 20 nM and 10 nM, respectively. It shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases and induces cell apoptosis with anti-tumor activity. It has limited blood-brain barrier permeability, mediated mainly by ABCB1[1][2][3][4][5][6]. It is supplied as an off-white to light yellow solid (C20H15ClF3N5, MW 417.81) at 99.56% purity.
Physical & Chemical Properties
| CAS Number | 1029044-16-3 |
|---|---|
| Molecular Formula | C20H15ClF3N5 |
| Molecular Weight | 417.81 g/mol |
| Purity | 99.56% |
| 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 |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (239.34 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (239.34 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 50% PEG400 + 50% PBS |
|---|---|
| Result | 10 mg/mL (23.93 mM); suspension; requires sonication |
Protocol 2
| Composition | 5% DMSO + 40% PEG300 + 5% Tween-80 + 50% saline |
|---|---|
| Result | 5 mg/mL (11.97 mM); suspension; requires sonication |
Protocol 3
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (4.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 4
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (4.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 5
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (4.98 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 6
| Composition | 0.5% CMC-Na/saline water |
|---|---|
| Result | 10 mg/mL (23.93 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
Pexidartinib (PLX-3397) is a potent, selective, ATP-competitive inhibitor of CSF1R (cFMS) and c-Kit. Its IC50s against FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC) are 160, 350, 860, 880, and 890 nM, respectively, which corresponds to 10- to 100-fold selectivity for c-Kit and CSF1R over these related kinases[1].
In Vivo
Pexidartinib can deplete microglia cells in mice. In adult male C57BL/6J mice (20-25 g), Pexidartinib (290 ppm in AIN-76A standard chow, 21 days) depletes brain microglia cells by 70%[5]. In C57BL/6J mice, Pexidartinib (600 ppm in chow, 10 days and 30 days) depletes more than 90% of brain microglia cells[6]. In neonatal mice, Pexidartinib (PLX3397; 0.25, 1 mg/kg, twice daily for 8 days) suppresses proliferation of microglia and BrdU-positive cells[2]. Pexidartinib (1 mg/kg, twice daily for 8 days) has no obvious effect on cleaved caspase-3-positive cells in mice[2]. In mice, Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) lowers tissue macrophage levels without affecting glucose homeostasis[4]. Pexidartinib shows limited blood-brain barrier permeability, mainly through ABCB1. Pexidartinib can mainly penetrate the damaged blood-brain barrier around the tumor, which lets tumor cells enter the intact blood-brain barrier.
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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