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Merck
CN
所有图片(2)

主要文件

428201

Sigma-Aldrich

LDN-211904

LDN-211904 modulates the biological activity of EphB3 receptor tyrosine kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate, EphB3 inhibitor, LDN-211904

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About This Item

经验公式(希尔记法):
C21H21ClN4O5
分子量:
444.87
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

方案

≥99% (HPLC)

表单

solid

效能

79 nM IC50

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 50 mg/mL, clear, nearly colorless

运输

ambient

储存温度

2-8°C

SMILES字符串

O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O

InChI

1S/C19H19ClN4O.C2H2O4/c20-15-3-1-2-4-16(15)23-19(25)17-11-22-18-6-5-14(12-24(17)18)13-7-9-21-10-8-13;3-1(4)2(5)6/h1-6,11-13,21H,7-10H2,(H,23,25);(H,3,4)(H,5,6)

InChI key

ODBJGLKPAQMCJA-UHFFFAOYSA-N

一般描述

A pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC50 of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.

生化/生理作用

Cell permeable: yes
Primary Target
Erythropoietin-producing hepatocellular carcinoma (Eph)
Reversible: yes

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett.19, 6122

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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