ASP5878 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

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ASP5878 {[allProObj[0].p_purity_real_show]}

货号：A494813

ASP5878 是一种口服活性的 FGFR 1、2、3 和 4 的抑制剂，IC50 值分别为 0.47 nM、0.6 nM、0.74 nM 和 3.5 nM，具有潜在的抗肿瘤活性。

ASP5878 化学结构
CAS号：1453208-66-6

ASP5878 3D分子结构
CAS号：1453208-66-6

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ASP5878 纯度/质量文件产品仅供科研

货号：A494813 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

FGFR 亚型比较

产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					99%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		99%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		c-Kit,FLT3	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		99%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				99%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

ASP5878 生物活性

靶点	FGFR2 FGFR2, IC50:0.6 nM FGFR3 FGFR3, IC50:0.74 nM FGFR4 FGFR4, IC50:3.5 nM FGFR1 FGFR1, IC50:0.47 nM
描述	ASP5878 is a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance.

ASP5878 细胞实验

Cell Line G636C-FGFR4/3T3 cells G636C-FGFR4/BaF3 cells ACH-iPSCs	Concentration	Treated Time	Description	References
G636C-FGFR4/3T3 cells	15.6 nM (IC50)	4 or 5 days	To evaluate the antiproliferative effect of ASP5878 on G636C-FGFR4/3T3 cells, showing sensitivity to ASP5878.	Sci Rep. 2019 Oct 10;9(1):14627.
G636C-FGFR4/BaF3 cells	34.4 nM (IC50)	4 or 5 days	To evaluate the antiproliferative effect of ASP5878 on G636C-FGFR4/BaF3 cells, showing sensitivity to ASP5878 in the absence of IL-3.	Sci Rep. 2019 Oct 10;9(1):14627.
ACH-iPSCs	10 nM	from day 15	Increased the expression levels of chondrocytic markers ACAN and COL2A1, resulting in the formation of cartilaginous particles.	Sci Rep. 2020 Dec 1;10(1):20915.

ASP5878 动物实验

Species Nude mice Mice	Animal Model Subcutaneous xenograft model with G636C-FGFR4/3T3 cells Fgfr3Ach transgenic mice	Administration	Dosage	Frequency	Description	References
Nude mice	Subcutaneous xenograft model with G636C-FGFR4/3T3 cells	Oral	3 mg/kg	Once daily for 8 days	To evaluate the antitumor activity of ASP5878 in a mouse xenograft model with G636C-FGFR4/3T3 cells, showing significant inhibition of tumor growth.	Sci Rep. 2019 Oct 10;9(1):14627.
Mice	Fgfr3Ach transgenic mice	Subcutaneous injection	300 μg/kg	Five times a week for 3 weeks	Evaluated the effect of ASP5878 on bone growth in ACH model mice, showing that 300 μg/kg ASP5878 significantly elongated the femur and tibia lengths in male mice.	Sci Rep. 2020 Dec 1;10(1):20915.

ASP5878 参考文献

[1]Kikuchi A, Suzuki T, et al. ASP5878, a selective FGFR inhibitor, to treat FGFR3-dependent urothelial cancer with or without chemoresistance. Cancer Sci. 2017 Feb;108(2):236-242.

[2]Futami T, Okada H, et al. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther. 2017 Jan;16(1):68-75.

ASP5878 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.55mL

4.91mL

2.45mL

ASP5878 技术信息

CAS号	1453208-66-6
分子式	C₁₈H₁₉F₂N₅O₄
分子量	407.37
SMILES Code	COC1=CC(OC)=C(F)C(COC2=CN=C(NC3=CN(CCO)N=C3)N=C2)=C1F
MDL No.	MFCD30532771

别名
运输	蓝冰

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 250 mg/mL(613.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

ASP5878 {[allProObj[0].p_purity_real_show]}

ASP5878 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

ASP5878 质控信息

ASP5878 生物活性

ASP5878 细胞实验

ASP5878 动物实验

ASP5878 参考文献

ASP5878 实验方案

ASP5878 技术信息

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FGFR2	FGFR2, IC50:0.6 nM
FGFR3	FGFR3, IC50:0.74 nM
FGFR4	FGFR4, IC50:3.5 nM
FGFR1	FGFR1, IC50:0.47 nM

ASP5878 {[allProObj[0].p_purity_real_show]}

ASP5878 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

ASP5878 质控信息

ASP5878 生物活性

ASP5878 细胞实验

ASP5878 动物实验

ASP5878 参考文献

ASP5878 实验方案

ASP5878 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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ASP5878 纯度/质量文件产品仅供科研