Molecular Weight(MW): 417.81
Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.
Cited by 16 Publications
6 Customer Reviews
Quantitative analyses of CSF-1R phosphorylation induced by CSF-1 in macrophages with (open column) and without (solid column) CSF1R c.1085A>G genetic variant. Macrophages differentiated from peripheral blood mononuclear cells were serum starved for 18 hours followed by stimulation with CSF-1 100 ng/mL for 5 minutes with or without pretreatment with CSF-1R inhibitor, PLX3397. The phosphorylation of CSF-1R was measured by phospho-MCSF-receptor sandwich ELISA Kit. Y axis, normalized CSF-1R phosphorylation. Each value represents mean ± SEM from at least seven different samples in each group.
Clin Cancer Res, 2017, 23(20):6021-6030. Pexidartinib (PLX3397) purchased from Selleck.
Microglia contribute to the protective effect of etifoxine. C57BL/6 mice received daily treatment of the colony stimulator factor 1 receptor inhibitor, PLX3397, for 21 days prior to 60 min MCAO. After MCAO and immediately at the onset of reperfusion, mice received a single i.p. injection of etifoxine or vehicle control. At 24 h after MCAO and reperfusion, neurodeficits and infarct volume were determined. a Bar graph shows numbers of CD11b+ CD45int cells in groups of MCAO mice receiving indicated treatments. b Bar graph shows numbers of CD11b+ CD45intTSPO+ cells in groups of MCAO mice receiving indicated treatments. c Bar graph shows numbers of CD11b+CD45high and CD11b−CD45high cells in groups of MCAO mice receiving indicated treatments. d Bar graph shows neurodeficits based on mNSS in MCAO mice receiving indicated treatments. e TTC-stained images show infarct in mice receiving etifoxine or vehicle after MCAO and reperfusion. f Bar graph shows infarct volume in MCAO mice receiving etifoxine or vehicle. n = 8 per group. Data were presented as mean ± SEM.
J Neuroinflammation, 2017, 14(1):151. Pexidartinib (PLX3397) purchased from Selleck.
Purity & Quality Control
Choose Selective CSF-1R Inhibitors
|Description||Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.|
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. 
|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.  In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion.  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.  In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. |
|In vitro||DMSO||83 mg/mL (198.65 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03291288||Active not recruiting||Drug: Tolbutamide|Drug: Midazolam|Drug: Pexidartinib||Drug Interaction Potential||Daiichi Sankyo Inc.||February 26 2018||Phase 1|
|NCT02975700||Active not recruiting||Drug: PLX3397||Melanoma||Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc.||January 2017||Not Applicable|
|NCT02777710||Active not recruiting||Drug: Pexidartinib|Drug: Durvalumab||Colorectal Cancer|Pancreatic Cancer|Metastatic Cancer|Advanced Cancer||Centre Leon Berard|AstraZeneca|Plexxikon||June 2016||Phase 1|
|NCT02071940||Unknown status||Drug: PLX3397||Malignant Melanoma||The Christie NHS Foundation Trust||October 2015||Phase 2|
|NCT02452424||Terminated||Drug: PLX3397|Biological: Pembrolizumab||Melanoma|Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck|Gastrointestinal Stromal Tumor (GIST)|Ovarian Cancer||Plexxikon|Merck Sharp & Dohme Corp.||July 2 2015||Phase 1|Phase 2|
|NCT02390752||Recruiting||Drug: PLX3397||Neurofibroma Plexiform|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Leukemia Prolymphocytic Acute|Sarcoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||April 29 2015||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
I am going to use PLX3397 for mice experiment. but I am not sure how to dissolve it, could you tell me the detail?
S7818 Pexidartinib (PLX3397) can dissolve in 5% DMSO+45% PEG 300+5% Tween 80+ddH2O at 10mg/ml.