6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮
| 中文名称 | 6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮 |
|---|---|
| 中文同义词 | 6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮;化合物 T15726 |
| 英文名称 | PyriMido[5',4':5,6]pyriMido[1,2-a]benziMidazol-5(6H)-one, 6-(2,6-diMethylphenyl)-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]- |
| 英文同义词 | PyriMido[5',4':5,6]pyriMido[1,2-a]benziMidazol-5(6H)-one, 6-(2,6-diMethylphenyl)-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]-;Lck Inhibitor;6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one;6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one |
| CAS号 | 847950-09-8 |
| 分子式 | C31H30N8O |
| 分子量 | 530.62 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 847950-09-8.mol |
| 结构式 | ![6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮 结构式](CAS/GIF/847950-09-8.gif) |
6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮 性质
| 沸点 | 809.1±75.0 °C(Predicted) |
|---|---|
| 密度 | 1.36±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 7.87±0.42(Predicted) |
Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC 50 =0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC 50 =0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT).
Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis.
Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the C
max
, AUC
0-∞
, t
max
and F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively.
| Animal Model: | Male Lewis rat (adjuvant-inducedarthritis model) |
| Dosage: | 0, 30, and 60 mg/kg |
| Administration: | P.o.; once daily; from day 9 today 17 |
| Result: | Showed a dose-dependent inhibition of arthritis, with an ED 50 estimated at 24 mg/kg. |
| Animal Model: | Sprague-Dawley Rats |
| Dosage: | P.o. (Pharmacokinetic Analysis) |
| Administration: | 5 mg/kg |
| Result: | The C max , AUC 0-∞ , t max and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12072 | Lck Inhibitor | 1 mg | 528元 | |
| 2024/04/30 | HY-12072 | 6-(2,6-二甲基苯基)-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-嘧啶并[5',4':5,6]嘧啶并[1,2-A]苯并咪唑-5(6H)-酮 Lck Inhibitor | 847950-09-8 | 5mg | 1162元 |