Pexidartinib hydrochloride (PLX-3397)

Modify Date: 2024-01-12 12:56:42

Pexidartinib hydrochloride (PLX-3397) structure	Common Name	Pexidartinib hydrochloride (PLX-3397)
	CAS Number	2040295-03-0	Molecular Weight	454.28
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₀H₁₆Cl₂F₃N₅	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Pexidartinib hydrochloride (PLX-3397)

Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively[1].

Name	Pexidartinib hydrochloride

Description	Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC50s of 160, 350, 860, 880, and 890 nM, respectively[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Fms Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Target	IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1]
In Vivo	Pexidartinib (PLX3397; 0.25, 1 mg/kg, i.p., twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice[2]. Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice[2]. Animal Model: Neonatal mice[2] Dosage: 0.25, 1 mg/kg Administration: I.P. twice daily for 8 days Result: Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells.
References	[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. [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.

Molecular Formula	C₂₀H₁₆Cl₂F₃N₅
Molecular Weight	454.28
Storage condition	2-8℃

DC Chemicals Limited
China
Product Name: Pexidartinib hydrochloride (PLX-3397)
Price: $200.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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