2035509-96-5
| 中文名称 | 2035509-96-5 |
|---|---|
| 中文同义词 | ERK5抑制剂(AX-15836);化合物AX-15836;2-((2-乙氧基-4-(4-(4-甲基哌嗪-1-基)哌啶-1-羰基)苯基)氨基)-5-甲基-11-(甲基磺酰基)-5,11-二氢-6H-苯并[E]嘧啶并[5,4-B][1,4]二氮杂卓-6-酮 |
| 英文名称 | AX-15836 |
| 英文同义词 | AX-15836;5,11-Dihydro-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5-methyl,11-(methylsulfonyl)-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one;6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-11-(methylsulfonyl)-;AX-15836,Extracellular signal regulated kinases,ERK,AX 15836,inhibit,Inhibitor,AX15836;2-((2-Ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5-methyl-11-(methylsulfonyl)-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one |
| CAS号 | 2035509-96-5 |
| 分子式 | C32H40N8O5S |
| 分子量 | 648.78 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂 |
| Mol文件 | 2035509-96-5.mol |
| 结构式 |  |
2035509-96-5 性质
| 沸点 | 848.9±75.0 °C(Predicted) |
|---|---|
| 密度 | 1.42±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：≥101mg/mL（155.68mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.14±0.42(Predicted) |
| 颜色 | 米白色至黄色 |
|
ERK5 8 nM (IC 50 ) |
AX-15836 shows more than 1,000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a K d of 3,600 nM. AX15836 shows similar intracellular potency (4–9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. AX15836 was completely ineffective (EC 50 >10 μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells.
安全信息
| 海关编码 | 2922500090 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-101846 | 2035509-96-5 AX-15836 | 2035509-96-5 | 5mg | 1500元 |
| 2024/08/19 | HY-101846 | 2035509-96-5 AX-15836 | 2035509-96-5 | 10mM * 1mLin DMSO | 2140元 |