Pexidartinib (PLX3397)

Catalog No.S7818

For research use only.

Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.

Pexidartinib (PLX3397) Chemical Structure

CAS No. 1029044-16-3

Selleck's Pexidartinib (PLX3397) has been cited by 79 publications

Purity & Quality Control

Choose Selective CSF-1R Inhibitors

Biological Activity

Description Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.
Targets
Kit [1]
(Cell-free assay)
CSF-1R [1]
(Cell-free assay)
Flt3 [1]
(Cell-free assay)
10 nM 20 nM 160 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
4T1 cells M4rkPGNmdGxidnnhZoltcXS7IHHzd4F6 MlLQNE4xOS1zMECgcocwdUx? M3vHe|I1KGh? M1\ZZ3Rz\WG2bXXueEB4cXSqIGDlfIll[XK2aX7pZkApOC5yMT2xNFAhdmdxbVypJIZweiB{NDDoc5VzeyCmaXSgco91KHOrZ37p[olk[W62bImgZYZn\WO2IH31dolv\SB2VEGgZ4Fz[2mwb33hJINmdGxiboXtZoVzKGmwII\peJJwKGG|IH3lZZN2emWmIHL5JINzgXO2YXygeolwdGW2IIP0ZYlvNg>? M4nNUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUO2O|M6Lz5|MEmzOlc{QTxxYU6=
Caco-2 cells NWX3XmJxS3m2b4TvfIlkcXS7IHHzd4F6 NWnrfGdVPDhiaB?= M4DWcWlEPTBiPTC1MlQ{KM7:TR?= MmTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|gyOzh5Mz:nQmNpTU2ETEyvZV4>
Caco-2 cells MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn;6OFghcA>? M1HlcWNEPTBiPTC0NU42OyEQvF2= NYD6PYRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzhzM{i3N{8oRkOqRV3CUFww[T5?
Assay
Methods Test Index PMID
Western blot p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R ; p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK 28932635 24718867
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. [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]

Protocol (from reference)

Animal Research:

[1]

  • Animal Models: MMTV-PyMT mice
  • Dosages: 40 mg/kg/day
  • Administration: p.o.

Solubility (25°C)

In vitro

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.

10mg/mL

Chemical Information

Molecular Weight 417.81
Formula

C20H15ClF3N5

CAS No. 1029044-16-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04703322 Recruiting Drug: Pexidartinib Tenosynovial Giant Cell Tumor Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. March 15 2021 Phase 2
NCT04635111 Recruiting Drug: TURALIO™ Hepatotoxicity|Tenosynovial Giant Cell Tumor Daiichi Sankyo Inc. January 7 2021 --
NCT04488822 Active not recruiting Drug: Pexidartinib Tenosynovial Giant Cell Tumor Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. September 2 2020 Phase 3
NCT04223635 Completed Drug: Pexidartinib Moderate Hepatic Impairment Daiichi Sankyo Inc. January 7 2020 Early Phase 1
NCT03291288 Completed Drug: Tolbutamide|Drug: Midazolam|Drug: Pexidartinib Drug Interaction Potential Daiichi Sankyo Inc. February 26 2018 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Frequently Asked Questions

Question 1:
I am going to use PLX3397 for mice experiment. but I am not sure how to dissolve it, could you tell me the detail?

Answer:
S7818 Pexidartinib (PLX3397) can dissolve in 5% DMSO+45% PEG 300+5% Tween 80+ddH2O at 10mg/ml.

Tags: buy Pexidartinib (PLX3397) | Pexidartinib (PLX3397) supplier | purchase Pexidartinib (PLX3397) | Pexidartinib (PLX3397) cost | Pexidartinib (PLX3397) manufacturer | order Pexidartinib (PLX3397) | Pexidartinib (PLX3397) distributor