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Pexidartinib hydrochloride (PLX-3397 HCl) is a selective, orally active, ATP-competitive CSF1R/M-CSFR inhibitor and c-Kit inhibitor with IC50 values of 20 and 10 nM, respectively, capable of inducing cancer cell apoptosis.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $38 | - | In Stock | |
| 10 mg | $53 | - | In Stock | |
| 25 mg | $87 | - | In Stock | |
| 50 mg | $123 | - | In Stock | |
| 100 mg | $156 | - | In Stock | |
| 500 mg | $372 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $43 | - | In Stock |
| Description | Pexidartinib hydrochloride (PLX-3397 HCl) is a selective, orally active, ATP-competitive CSF1R/M-CSFR inhibitor and c-Kit inhibitor with IC50 values of 20 and 10 nM, respectively, capable of inducing cancer cell apoptosis. |
| Targets&IC50 | FLT3:160 nM, cFMS:20 nM, KDR:350 nM, LCK:860 nM, FLT1:880 nM, c-Kit:10 nM, NTRK3:890 nM |
| In vitro | Pexidartinib hydrochloride is a highly potent, selective, ATP-competitive inhibitor of CSF1R (cFMS) and c-Kit. It exhibits 10–100 times greater inhibitory selectivity for c-Kit and CSF1R compared to other related kinases (such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1), and NTRK3 (TRKC)), with IC50 values of 160 nM, 350 nM, 860 nM, 880 nM, and 890 nM, respectively [1]. |
| In vivo | In the neonatal mouse model, Pexidartinib hydrochloride (0.25 and 1 mg/kg, intraperitoneal injection, twice daily for 8 days) inhibited the proliferation of microglia and BrdU-positive cells [2]. Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 days) did not significantly affect the number of cleaved caspase-3-positive cells in mice [2]. Pexidartinib hydrochloride (50 mg/kg, oral administration, once every two days for 3 weeks) reduced macrophage levels in mouse tissues without interfering with Vitis vinifera glucose homeostasis [4]. |
| Synonyms | PLX-3397 hydrochloride, PLX3397 hydrochloride |
| Molecular Weight | 454.28 |
| Formula | C20H16Cl2F3N5 |
| Cas No. | 2040295-03-0 |
| Smiles | Cl.FC(F)(F)C1=NC=C(C=C1)CNC2=NC=C(C=C2)CC3=CNC=4N=CC(Cl)=CC43 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble) DMSO: 48 mg/mL (105.66 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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