Pexidartinib (PLX3397)

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

Keywords

Pexidartinib PLX3397 1029044-16-3

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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	Activity Description	PMID
4T1 cells	Cell viability assay	0.01-100 ng/mL	24 h	Treatment with Pexidartinib (0.01-100 ng/mL) for 24 hours did not significantly affect murine 4T1 carcinoma cell number in vitro as measured by crystal violet stain.	30936739
Caco-2 cells	Cytotoxicity assay		48 h	IC50 = 5.43 μM	ChEMBL
Caco-2 cells	Cell Viability Assay		48 h	CC50 = 41.53 μM	ChEMBL

Assay

Methods	Test Index	PMID
Western blot	p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK; p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R;	24718867 28932635

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]

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