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LDN-211904
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDN-211904图片
CAS NO:1198408-78-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt444.9
Cas No.1198408-78-4
FormulaC19H19ClN4O·C2H2O4
Solubility≤20mg/ml in DMSO;0.5mg/ml in dimethyl formamide
Chemical NameN-(2-chlorophenyl)-6-(4-piperidinyl)-imidazo[1,2-a]pyridine-3-carboxamide, monoethanedioate
Canonical SMILESO=C(NC1=C(Cl)C=CC=C1)C2=CN=C(C=C3)N2C=C3C4CCNCC4.OC(C(O)=O)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

IC50: 79 nM for EphB3

LDN-211904 is an inhibitor of erythropoietin-producing hepatocellular carcinoma (Eph) receptors.

Erythropoietin-producing hepatocellular carcinoma (Eph) receptors, a group of highly conserved transmembrane proteins composed of multiple domains, participate in various cell signaling pathways. So far, 16 Eph receptors have been identified in vertebrates, which can be divided into two major classes (EphA and EphB) based on sequence similarity. Mammals including humans have 14 Eph receptors (EphA1–EphA8, EphA10, EphB1–EphB4 and EphB6).

In vitro: Previous study found that LDN-211904, a 4-piperidinyl analog, retained significant EphB3 inhibitory activity, and also had greater aqueous solubility due to the presence of a basic amine. LDN-211904 was profiled for functional inhibitory activity against a panel of 288 kinases and the results showed that LDN-211904 was quite selective for tyrosine kinases. The only noted exceptions were the three serine/threonine kinases p38a, p38b, and Qik. In addition, only LDN-211904 showed moderate selectivity among the tyrosine kinases and little selectivity verses other EphA and EphB subtypes, except for EphA6 and EphA7. Moreover, LDN-211904 demonstrated the best stability with a t1/2 of 348 min and a CLint of 4 μL/min/mg protein [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Qiao, L. ,Choi, S.,Case, A., et al. Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors. Bioor. Med. Chem. Lett. 19(21), 6122-6126 (2009).