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- 2025年12月05日
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| 规格： | 10 mM * 1 mL | 产品价格： | ￥923.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥406.0 |
| 规格： | 5 mg | 产品价格： | ￥960.0 |
| 规格： | 10 mg | 产品价格： | ￥1325.0 |
| 规格： | 25 mg | 产品价格： | ￥2238.0 |
| 规格： | 50 mg | 产品价格： | ￥3288.0 |
| 规格： | 100 mg | 产品价格： | ￥4700.0 |
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PF-5274857
CAS No. : 1373615-35-0
MCE 国际站：PF-5274857
产品活性：PF-5274857 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，Ki 值为 4.6 nM。PF-5274857 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 (T1/2) of 1.7±0.1 hours.
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文献和实验日本VESSEL（威威）GT-P6EXD,GT-P6EXD(A
4TS,GT-S4TR GT-S5TFG/S5TFB/S5TFR/S5TG/S5TB/S5TR/S5TR/S5TS,GT-1600VP/1600VPL/1600VPH/1600VPHL GT-3800VP/3800V/3800VL/3900VL/4800VL,GT-2000PF/2500PF/2500LF/3800PF/3800LF/4200PF GT-4200LF,GT-S55R,GT-S650/P6IIZ/S600C/P8II/P12
的control载体。它含有氯素酶转乙酰基酶（CAT）基因，作为监控蛋白表达、纯化和加工条件的手段。载体都是利用tac启动子，它由lac启动子的-10区和trp启动子-35区融合而成，汇合了lac和trp两者优点，是一个很强的启动子，同样受LacI阻遏蛋白调控。产量据说通常可以达到1―5mg/L。用SoftLink™抗生物素蛋白亲和纯化树脂是专利技术，可将蛋白质以非变性形式洗脱出来。或者也可以利用TetraLink™ 四联抗生物素蛋白树脂对蛋白进行纯化。PinPoint 载体的特点是含有编码内源蛋白酶因子Xa
Tissue Processing and Sectioning
of formaldehyde to formic acid. Because of the preservative, NBF has a shelf life of months, whereas 4% PF must be made fresh. Optimal histology requires adequate fixation, about 48 hrs at room temperature for thinly sliced tissues. Inadequately fixed tissues
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