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Pexidartinib

Catalog No. T2115 CAS 1029044-16-3

Synonyms: PLX-3397

Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.

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Pexidartinib, CAS 1029044-16-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 40.00
10 mg	In stock	$ 56.00
25 mg	In stock	$ 87.00
50 mg	In stock	$ 123.00
100 mg	In stock	$ 156.00
200 mg	In stock	$ 213.00
500 mg	In stock	$ 369.00
1 mL * 10 mM (in DMSO)	In stock	$ 44.00

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Purity: 99.66%

Purity: 99.51%

Purity: 99.4%

Purity: 99.21%

Purity: 98.59%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
Targets&IC50	FLT3:160 nM, c-Kit:10 nM, CSF1R:20 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]
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?Ly6 g?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]
Kinase Assay	Competitive binding fluorescent polarization assay: Recombinant Hsp90β, TAMRA-radicicol, or various concentrations of NVP-BEP800 is added in assay buffer (50 mM TRIS pH 7.4, 5 mM MgCl2, 150 mM KCl, and 0.1% CHAPS), mixed, and incubated at room temperature for 30 to 45 minutes prior to reading. The 2D-FIDA-based HTS assay based on confocal technologies monitors the decreased fluorescence polarization on displacement of the high affinity ligand TAMRA-radicicol from Hsp90β by NVP-BEP800. The concentration of NVP-BEP800 which inhibits Hsp90β by 50% is determined from the competition curve.

Synonyms	PLX-3397
Molecular Weight	417.81
Formula	C20H15ClF3N5
CAS No.	1029044-16-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 77 mg/mL (184.3 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. DeNardo DG, et al. Cancer Discov. 2011, 1(1), 54-67. 2. Coniglio SJ, et al. Mol Med. 2012, 18, 519-527. 3. Chitu V, et al. Blood. 2012, 120(15), 3126-3135. 4. Sluijter M, et al. PLoS One. 2014, 9(8), e104230. 5. Fan K, Li Y, Wang H, et al. Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior[J]. Cell. 2019, 179(4): 864-879. e19.

Citations

1. Fan K, Li Y, Wang H, et al. Stress-Induced Metabolic Disorder in Peripheral CD4+ T Cells Leads to Anxiety-like Behavior. Cell. 2019, 179(4): 864-879. e19. 2. Xu F, Han L, Wang Y, et al.Prolonged anesthesia induces neuroinflammation and complement-mediated microglial synaptic elimination involved in neurocognitive dysfunction and anxiety-like behaviors.BMC medicine.2023, 21(1): 1-27.

Related compound libraries

This product is contained In the following compound libraries：

FDA-Approved Kinase Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library EMA Approved Drug Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pexidartinib 1029044-16-3 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors c-Fms FLT CSF-1R c-Kit inhibit CSF-1 receptor SCFR Inhibitor PLX 3397 PLX3397 colony stimulating factor 1 receptor CSF1R CD117 PLX-3397 inhibitor

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