PF-5274857,1613439-62-5

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PF-5274857 hydrochloride

CAS No. : 1613439-62-5

MCE 国际站：PF-5274857 hydrochloride

产品活性：PF-5274857 hydrochloride 是一种有效的、选择性的、具有口服活性和可透过血脑屏障的 Smo 拮抗剂，IC₅₀ 值为 5.8 nM，K_i 值为 4.6 nM。PF-5274857 hydrochloride 有潜力用于包括激活的 Hh 途径驱动的脑肿瘤和脑转移在内的多种肿瘤的研究。

研究领域：Stem Cell/Wnt

作用靶点：Smo

In Vitro: PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC₅₀ of 2.7±1.4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells.
PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM.

In Vivo: PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models.
PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose.
PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor.
PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch^+/− p53^−/− medulloblastoma mice.
PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T_1/2) of 1.7±0.1 hours.

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