LDN-211904
(Synonyms: N-(2-氯苯基)-6-(4-哌啶基)-咪唑并[1,2-A]吡啶-3-甲酰胺草酸盐) 目录号 : GC16798An EphB3 kinase inhibitor
Cas No.:1198408-78-4
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 1198408-78-4 | SDF | |
| 别名 | N-(2-氯苯基)-6-(4-哌啶基)-咪唑并[1,2-A]吡啶-3-甲酰胺草酸盐 | ||
| 化学名 | N-(2-chlorophenyl)-6-(4-piperidinyl)-imidazo[1,2-a]pyridine-3-carboxamide, monoethanedioate | ||
| Canonical SMILES | O=C(NC1=C(Cl)C=CC=C1)C2=CN=C(C=C3)N2C=C3C4CCNCC4.OC(C(O)=O)=O | ||
| 分子式 | C19H19ClN4O • C2H2O4 | 分子量 | 444.9 |
| 溶解度 | ≤20mg/ml in DMSO;0.5mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2477 mL | 11.2385 mL | 22.477 mL |
| 5 mM | 0.4495 mL | 2.2477 mL | 4.4954 mL |
| 10 mM | 0.2248 mL | 1.1238 mL | 2.2477 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet