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)和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。

Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC 50 s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity [1].

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 IC 50 s of 160, 350, 860, 880, and 890 nM, respectively [1].

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 [2]. Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice [2]. Pexidartinib hydrochloride (50 mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice [4]. Animal Model: Neonatal mice [2] Dosage: 0.25, 1 mg/kg Administration: I.P. twice daily for 8 days Result: Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells. Animal Model: 10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice) [4] Dosage: 50 mg/kg Administration: P.o.; every second day for 3 weeks Result: Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels.

2040295-03-0

C20H16Cl2F3N5

454.28

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years