1276121-88-0
1276121-88-0 结构式
基本信息
(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
MK2 INHIBITOR
(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
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)-
物理化学性质
| 报价日期 | 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 |
| 2024/04/30 | HY-107427 | PF-3644022 PF-3644022 | 1276121-88-0 | 10mM * 1mLin DMSO | 3960元 |
常见问题列表
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. |