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。
别名：ASP-5878
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.
| 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 |
| 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。 |
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 |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 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。
| 其他相关的FGFR产品 |
|---|
| Bemarituzumab
Bemarituzumab (FPA144) is a first-in-class, humanized, afucosylated immunoglobulin G1 monoclonal antibody (mAb) directed against fibroblast growth factor receptor 2b (FGFR2b) with two mechanisms of action against FGFR2b-overexpressing tumors: inhibition of FGFR2b signaling and enhanced antibody-dependent cell-mediated cytotoxicity (ADCC). |
| WAY-625530
WAY-625530 is a Fibroblast Growth Factor Receptor 1 Kinase inhibitor. |
| WAY-621856
WAY-621856 is a FGFR inhibitor. |
| WAY-603814
WAY-603814 is a FGFR1 inhibitor |
| WAY-600868
WAY-600868 is a FGFR3 inhibitor. |
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