Pexidartinib - PLX 3397

Based on 16 reference(s) in Google Scholar 9 10 16

Axon 2501

CAS [1029044-16-3]

MF C20H15ClF3N5
MW 417.81

Purity: 99%
Soluble in DMSO

Pexidartinib

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.

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.

Angiogenesis Cell Signaling & Oncology CNS Stem Cell FLT3 TGF-β MAPK JAK-STAT PI3K-Akt-mTOR c-KIT RTK class III and IV; EC 2.7.10.1 CSF1R

Mutil-targeted RTK inhibitor of CSF1R, c-Kit, and FLT3

Chemical name

5-((5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)pyridin-2-amine

Parent CAS No.

[1029044-16-3]

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