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Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $40 | In Stock | |
10 mg | $56 | In Stock | |
25 mg | $87 | In Stock | |
50 mg | $123 | In Stock | |
100 mg | $156 | In Stock | |
200 mg | $213 | In Stock | |
500 mg | $369 | In Stock | |
1 mL x 10 mM (in DMSO) | $44 | In Stock |
Description | Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity. |
Targets&IC50 | FLT3:160 nM, c-Kit:10 nM, CSF1R:20 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?Ly6 g?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] |
Kinase Assay | Competitive binding fluorescent polarization assay: Recombinant Hsp90β, TAMRA-radicicol, or various concentrations of NVP-BEP800 is added in assay buffer (50 mM TRIS pH 7.4, 5 mM MgCl2, 150 mM KCl, and 0.1% CHAPS), mixed, and incubated at room temperature for 30 to 45 minutes prior to reading. The 2D-FIDA-based HTS assay based on confocal technologies monitors the decreased fluorescence polarization on displacement of the high affinity ligand TAMRA-radicicol from Hsp90β by NVP-BEP800. The concentration of NVP-BEP800 which inhibits Hsp90β by 50% is determined from the competition curve. |
Alias | PLX-3397 |
Molecular Weight | 417.81 |
Formula | C20H15ClF3N5 |
Cas No. | 1029044-16-3 |
Smiles | FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 |
Relative Density. | 1.458 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (107.7 mM), Sonication is recommended. ![]() Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 7.7 mg/mL (18.43 mM), suspension.In vivo: Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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