产品说明
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.
包装
5 mg in Glass bottle
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
基本信息
| 经验(实验)分子式 | C21H21ClN4O5 |
| 分子量 | 444.87 |
| MDL编号 | MFCD28023573 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥99% (HPLC) |
| 形式 | solid |
| 效能 | 79 nM IC50 |
| manufacturer/tradename | 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℃ |
| SMILES string | O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
