PD-166866 | FGFR1 Inhibitor | AmBeed-信号通路专用抑制剂

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PD-166866 98%

货号：A339638

PD 166866 is a selective FGFR tyrosine kinase inhibitor with an IC50 of 52.4 nM.

PD-166866 化学结构
CAS号：192705-79-6

PD-166866 3D分子结构
CAS号：192705-79-6

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PD-166866 纯度/质量文件产品仅供科研

货号：A339638 标准纯度： 98% 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

FGFR 亚型比较
自噬亚型比较

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					98%
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		98%
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		98%
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			✔				98%
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。

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
Lys05	✔		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。

PD-166866 生物活性

靶点	FGFR1 FGFR1, IC50:52.4 nM
描述	The FGFR (fibroblast growth factor receptor) family comprises four members, FGFR1, FGFR2, FGFR3 and FGFR4, ligand of which can induce cellular phosphorylation events, proliferation and potent antiangiogenic activity. PD166866 is a highly selective and nanomolar potent inhibitor of FGFR-1 tyrosine kinase with an IC50 value of 52.4nM (measure protein tyrosine kinase activity) and no effect on c-Src, platelet-derived growth factor receptor-b, EGFR or insulin receptor tyrosine kinases or on MAPK, PKC and CDK4 at concentrations as high as 50μM. Pre-treatment with PD 166866 on concentration of 10 or 100nM for 2h caused inhibition on autophosphorylation of FGFR1 induced by bFGF (25ng/ml) for 5 min in NIH 3T3 cells expressing endogenous FGFR1 and in L6 cells overexpressing the human FGFR1 tyrosine kinase, along with the inhibition of downstream p-ERK 1/2. Consistent with this, daily exposure to PD 166866 at concentrations 1-100nM for 8 consecutive days resulted in a concentration-related inhibition of bFGF-stimulated cell growth of L6 cells^[1]. Another mechanism action of PD166866 on negative control of cell proliferation maybe due to its activation of the apoptotic pathway, suggested by specific point as evaluation of DNA damage, lipoperoxidation of the cell membrane and increase of expression of PARP, an enzyme directly involved in DNA repair^[2].
作用机制	PD 166866 is an ATP competitive inhibitor of FGFR1.^[1]

PD-166866 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HUVEC cells		Function assay		Inhibition of microcapillary growth in HUVEC cells, IC50=0.1 μM	11063616

PD-166866 动物研究

Dose	Mice^[3] (i.p.): 20 mg/kg
Administration	i.p.

PD-166866 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.22mL

5.04mL

2.52mL

PD-166866 技术信息

CAS号	192705-79-6
分子式	C₂₀H₂₄N₆O₃
分子量	396.443

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 3 mg/mL(7.57 mM)，配合低频超声，并水浴加热至45℃助溶，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

动物实验配方

4% DMSO+30% PEG 300+2% Tween 80+water 4 mg/mL

PD-166866 98%

PD-166866 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

PD-166866 质控信息

PD-166866 生物活性

PD-166866 细胞研究

PD-166866 动物研究

PD-166866 实验方案

PD-166866 技术信息

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PD-166866 98%

PD-166866 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

PD-166866 质控信息

PD-166866 生物活性

PD-166866 细胞研究

PD-166866 动物研究

PD-166866 实验方案

PD-166866 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

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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PD-166866 纯度/质量文件产品仅供科研