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Pexidartinib
- PLX 3397
- Soluble in DMSO
- MF: C20H15ClF3N5
- MW: 417.81
Description
Multi-targeted receptor tyrosine kinase inhibitor of CSF1R, c-Kit, and FLT3 (IC50 values 13 nM, 27 nM, and 11 nM, respectively) Administration of PLX3397 reduced CIBP, induced substantial intratumoral fibrosis, and was also highly efficacious in reducing tumor cell growth, formation of new tumor colonies in bone, and pathological tumor-induced bone remodeling. PLX3397 is superior to imatinib in the treatment of malignant peripheral nerve sheath tumor (MPNST), and the combination of PLX3397 with a TORC1 inhibitor could provide a new therapeutic approach for the treatment of this disease.
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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