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.
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|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:
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:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*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||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02390752||Recruiting||Neurofibroma, Plexiform|Precursor Cell Lymphoblastic Leukemia-Lymphoma|Leukemia, Prolymphocytic, Acute|Sarcoma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||March 6, 2015||Phase 1|Phase 2|
|NCT02975700||Not yet recruiting||Metastatic Melanoma||Plexxikon||January 2017||Phase 1|Phase 2|
|NCT02777710||Recruiting||Colorectal Cancer|Pancreatic Cancer|Metastatic Cancer|Advanced Cancer||Centre Leon Berard|AstraZeneca|Plexxikon||June 2016||Phase 1|
|NCT02734433||Recruiting||Advanced Solid Tumors||Daiichi Sankyo Co., Ltd.|Quintiles, Inc.|Daiichi Sankyo Inc.||June 2016||Phase 1|
|NCT02071940||Recruiting||Malignant Melanoma||The Christie NHS Foundation Trust||October 2015||Phase 2|
|NCT02452424||Recruiting||Melanoma|Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck|GIST||Plexxikon|Merck Sharp & Dohme Corp.||June 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 10% DMSO/40% PEG 300/ddH2O at 15mg/ml clearly.