Pexidartinib

CAS No. : 1029044-16-3

MCE 站：Pexidartinib

产品活性：Pexidartinib (PLX-3397) 是一种有效的，具有口服活性的、选择性ATP-竞争性的集落刺激因子 1 (CSF1R 或 M-CSFR) 和 c-Kit 抑制剂，IC₅₀ 值分别为 20 和 10 nM。Pexidartinib (PLX-3397) 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 890 nM。Pexidartinib (PLX-3397) 可以诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：c-Fms  |  c-Kit  |  Apoptosis

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.

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.
Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice.
Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice.

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