Formulation: A solid
Formal Name: (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
Purity: ≥95%
Formula Markup: C21H18N4OS
Formula Weight: 374,5
Shelf life (days): 1460
CAS Number: 1276121-88-0
Notes: PF-3644022 is an inhibitor of MAPK-activated protein kinase 2 (MK2; IC50 = 5.2 nM).{65720} It is selective for MK2 over MK3, MAPK-interacting protein kinase 1 (MNK-1), MNK-2, p90 ribosomal S6 kinase 1 (MSK1), MSK2, and p90 ribosomal S6 kinases 1-4 (RSK1-4; IC50s = 53, 3,000, 148, >1,000, >1,000, and >1,000 nM, respectively), as well as a panel of 200 other kinases at 1 µM, but also inhibits MK5/PRAK (IC50 = 5 nM). PF-3644022 inhibits LPS-induced TNF-α production in U937 cells and isolated human peripheral blood mononuclear cells (PBMCs) and whole blood (IC50s = 0.159, 0.16, and 1.97 µM, respectively) and reduces paw swelling in a rat model of arthritis induced by streptococcal cell wall peptidoglycan–polysaccharide complexes (ED50 = 20 mg/kg). It prevents decreases in motor function in a twy/twy mouse model of chronic cervical spinal cord compression when administered at a dose of 30 mg/kg.{65721} Peritumoral administration of PF-3644022 (30 µl of a 50 µM solution) enhances radiation-induced decreases in tumor volume and increases in survival in a patient-derived xenograft (PDX) mouse model of head and neck squamous cell carcinoma (HNSCC).{65722}
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