Pexidartinib hydrochloride | MedChemExpress (MCE)-产品咨询-资讯-生物在线

Pexidartinib hydrochloride | MedChemExpress (MCE)

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Pexidartinib hydrochloride

CAS No. : 2040295-03-0

MCE 国际站:Pexidartinib hydrochloride

产品活性:Pexidartinib hydrochloride (PLX-3397 hydrochloride) 是一种有效、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)c-Kit 抑制剂,IC50 值分别为 20 和 10 nM。Pexidartinib hydrochloride 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 hydrochloride 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 hydrochloride (PLX-3397 hydrochloride) 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 can be used to deplete the microglia cells in mice.
Pexidartinib (290 ppm in AIN-76A standard chow, 21 days) depletes the microglia cells in brain by 70% in adult male C57BL/6 J mice (20–25 g).
Pexidartinib (600 ppm in chow, 10 days and 30 days ) depletes the microglia cells more than 90% in brain of C57BL/6J mice.
Pexidartinib hydrochloride (0.25, 1 mg/kg, i.p., twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice.
Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice.
Pexidartinib hydrochloride (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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