Pexidartinib hydrochloride (Cat No.:I019324) is a potent and selective inhibitor of the tyrosine kinase receptor, particularly the colony-stimulating factor 1 receptor (CSF1R). By targeting CSF1R, Pexidartinib hydrochloride interferes with the signaling pathways involved in the growth and survival of certain cells, particularly those involved in the tumor microenvironment. This drug has been approved for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT) that is not amenable to improvement with surgery. Pexidartinib hydrochloride offers a valuable therapeutic option for patients with this rare and debilitating tumor, potentially improving their quality of life and reducing the need for invasive interventions.
| Catalog Number | I019324 |
| CAS Number | 2040295-03-0 |
| Molecular Formula | C₂₀H₁₆Cl₂F₃N₅ |
| Purity | ≥95% |
| IUPAC Name | 5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine;hydrochloride |
| InChI | InChI=1S/C20H15ClF3N5.ClH/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);1H |
| InChIKey | CJLUYLRKLUYCEK-UHFFFAOYSA-N |
| SMILES | C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F.Cl |
| Reference | [1]. DeNardo DG, et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67.<br>[2]. Kuse Y, et al. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018.<br>[3]. Lee JH, et al. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2.<br>[4]. Merry TL, et al. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2020;44(1):245-253. |
