Pexidartinib hydrochloride |
| Catalog No.GC34708 |
Le chlorhydrate de pexidartinib (chlorhydrate de PLX-3397) est un puissant récepteur du facteur 1 de stimulation des colonies (CSF1R ou M-CSFR) et un inhibiteur de c-Kit puissants, actifs par voie orale, sélectifs et compétitifs pour l'ATP, avec des IC50 de 20 et 10 nM, respectivement. Le chlorhydrate de pexidartinib présente une sélectivité de 10 À 100 fois pour c-Kit et CSF1R par rapport À d'autres kinases apparentées. Le chlorhydrate de pexidartinib induit l'apoptose cellulaire et a une activité anticancéreuse.
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Cas No.: 2040295-03-0
Sample solution is provided at 25 µL, 10mM.
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]. IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)[1]
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]
[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.
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