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ASP5878

目录号 M10518 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


ASP5878是一种新型的选择性的FGFR抑制剂,对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为0.47, 0.60, 0.74和3.5 nM。

ASP5878结构式

别名:ASP-5878

包装 价格 库存状态
5mg 原价 ¥ 2320
促销价 ¥ 2204
中国库存现货
10mg 原价 ¥ 4000
促销价 ¥ 3800
中国库存现货
其他规格数量报价?

质量标准及产品资料
生物活性

ASP5878 is a novel selective FGFR inhibitor with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3 and 4, respectively. ASP5878 inhibits the cell proliferation of HCC cell lines expressing FGF19. ASP5878 inhibits FGFR4 phosphorylation and its treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation in Hep3B2.1-7 cells.

In vivo, ASP5878 (3 mg/kg; oral administration) induces sustained tumor regression in a subcutaneous xenograft mouse model using Hep3B2.1-7. In HuH-7, an orthotopic xenograft mouse model, ASP5878 induces complete tumor regression and dramatically extended the survival of the mice.

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验
细胞系 Human HCC cell lines
方法 HCC cell lines were cultured according to each manufacturer’s guideline. The cell lines in this study were not authenticated by any tests in our laboratory but were purchased from the providers of authenticated cell lines and stored at early passages in a central cell bank at Astellas Pharma Inc. The experiments were conducted using low-passage cultures of these stocks. The cells were seeded in 96-well plates and incubated overnight. The cells were treated with ASP5878 for 5 days. Cell viability was measured using CellTiter-GloTM (Promega, Madison, WI).
浓度 0-1000 nM
处理时间 5 days
动物实验
动物模型 HCC orthotopic xenograft model
配制 Cremophor EL/ethanol or 0.5% MC
剂量 3 mg/kg
给药处理 oral
化学数据
分子量 407.37
分子式 C18H19F2N5O4
CAS号 1453208-66-6
溶解性(25°C) DMSO ≥ 80 mg/mL
储存条件 粉末型式       -20°C   3年;4°C   2年
溶于溶剂       -80°C   6个月;-20°C   1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
储备液配制

以下数据基于产品分子量,对于具体产品,请根据在不同溶剂中的溶解度和COA中的说明进行操作。

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.491 mL 2.4548 mL 4.9095 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 mL
不同实验动物依据体表面积的等效剂量转换表(参考来源于公开文献
小鼠 大鼠 豚鼠 仓鼠
重量 (kg) 0.02 0.15 1.8 0.4 0.08 10
体表面积 (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km 系数 3 6 12 8 5 20
动物 A (mg/kg) = 动物 B (mg/kg) ×  动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Aya Kikuchi, et al. Cancer Sci. ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance

[2] Takashi Futami, et al. Mol Cancer Ther. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma

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