PF-3644022
| 中文名称 | PF-3644022 |
|---|---|
| 中文同义词 | (R)-10-甲基-3-(6-甲基吡啶-3-基)-9,10,11,12四氢-8H-[1,4]二氮杂卓并[5',6':4,5]噻吩并[3,2-F]喹啉-8-酮;化合物PF-3644022;PF-3644022 水合物;PF 3644022,MK2抑制剂;(R)-10-甲基-3-(6-甲基吡啶-3-基)-9,10,11,12四氢-8H-[1,4]二氮杂卓并[5',6':4,5]噻吩并[3,2-F]喹啉-8-酮 |
| 英文名称 | PF 3644022 |
| 英文同义词 | PF 3644022;(10R)-9,10,11,12-Tetrahydro-10-Methyl-3-(6-Methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one;MK2 INHIBITOR;8H-[1,4]Diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one, 9,10,11,12-tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-, (10R)-;(R)-10-Methyl-3-(6-methylpyridin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one;MAPKAP kinase 2,monocytic,lipopolysaccharide,IL-6,TNFα,safety,Anti-inflammatory,PF3644022,orally,PRAK,efficacious,inhibit,PF-3644022,Mitogen-activated protein kinase activated protein kinase 2,p38 MAPK,Inhibitor,MK3,MAP kinase activated protein kinase 2,MAPKAPK2 (MK2),MAPK activated protein kinase 2,PF 3644022;(R)-10-Methyl-3-(6-methylpyridin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one |
| CAS号 | 1276121-88-0 |
| 分子式 | C21H18N4OS |
| 分子量 | 374.46 |
| EINECS号 | |
| 相关类别 | Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 1276121-88-0.mol |
| 结构式 |  |
PF-3644022 性质
| 熔点 | >180°C (dec.) |
|---|---|
| 沸点 | 703.3±60.0 °C(Predicted) |
| 密度 | 1.298±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.51±0.40(Predicted) |
| 颜色 | 灰白色至黄色 |
IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3).
Ki: 3 nM (MK2)
The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an
IC
50
of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2.
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (
IC
50
of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with
IC
50
values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity.
PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED 50 value of 20 mg/kg.
| Animal Model: | Female Lewis rats (125-140 g) injected with streptococcal cell wall |
| Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg |
| Administration: | Oral gavage; twice a day; for 12 days |
| Result: | Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing. |
安全信息
| 海关编码 | 2934999090 |
|---|
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-107427 | PF-3644022 PF-3644022 | 1276121-88-0 | 1mg | 1440元 |
| 2024/04/30 | HY-107427 | PF-3644022 PF-3644022 | 1276121-88-0 | 5mg | 3400元 |