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Pexidartinib
- PLX 3397
- Soluble in DMSO
- MF: C20H15ClF3N5
- MW: 417.81
Description
Pexidartinib (PLX3397) is a multi-target receptor tyrosine kinase inhibitor with potent activity at CSF1R, c-Kit and FLT3. It suppresses macrophage lineage signaling and tumor microenvironment pathways driven by colony-stimulating factor 1.
CSF1R signaling supports macrophage survival, differentiation and recruitment in tumors, inflammation and bone disease. Pexidartinib is useful for studying tumor-associated macrophages, CSF1R biology and kinase-driven oncology models.
Key Features
- CSF1R/c-Kit/FLT3 receptor tyrosine kinase inhibitor
- Reported IC50 values: 13 nM for CSF1R, 27 nM for c-Kit and 11 nM for FLT3
- Modulates macrophage and tumor microenvironment signaling
- Clinically validated CSF1R-targeted pharmacology
Applications
- CSF1R kinase pharmacology
- Tumor-associated macrophage research
- Cancer and inflammatory microenvironment models
- FLT3 and c-Kit pathway studies
More Information
| Parent CAS No. | 1029044-16-3 |
|---|---|
| Chemical Name | 5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine |
| SMILES | C1(Cl)C=C2C(CC3C=CC(NCC4C=CC(C(F)(F)F)=NC=4)=NC=3)=CNC2=NC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29) |
| InChiKey | JGWRKYUXBBNENE-UHFFFAOYSA-N |
| CID | 25151352 |
| Short Description | RTK inhibitor |
References
- C.C. Smith et al. Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397. Cancer Discov. 2015 Jun;5(6):668-79.
- P.P. Patwardhan et al. Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs. Clin Cancer Res. 2014 Jun 15;20(12):3146-58.
- T.S. Kim et al. Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor. Clin Cancer Res. 2014 May 1;20(9):2350-62.
- M.L. Thompson et al. Targeting cells of the myeloid lineage attenuates pain and disease progression in a prostate model of bone cancer. Pain. 2015 Sep;156(9):1692-702.
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