Pexidartinib

1029044-16-3

C20H15ClF3N5

DMSO : 5 mg/mL (11.97 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Protein Tyrosine Kinase/RTK; Protein Tyrosine Kinase/RTK

Pexidartinib (PLX-3397) 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. Anti-tumor activity^[1]. IC50 & 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 Vitro: Pexidartinib (PLX-3397) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, shows 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]. In Vivo: Pexidartinib (PLX3397; 0.25, 1 mg/kg, 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].