Pexidartinibhydrochloride(PLX-3397hydrochloride)是一种有效、选择性、ATP-竞争性的CSF1R(cFMS)和c-Kit抑制剂，IC50值分别为20和10nM。Pexidartinib对c-Kit和CSF1R的选择性是对其他相关激酶的10-100倍，例如FLT3，KDR(VEGFR2)，LCK，FLT1(VEGFR1)和NTRK3(TRKC)，IC50值分别为160，350，860，880和890nM。
CAS：2040295-03-0
分子式：C20H16Cl2F3N5
分子量：454.28
纯度：98%
存储：Store at -20°C

Background:

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.