产品描述:
SCIO 469 is a p38 MAPK inhibitor (IC50 = 9 nM for p38α).{48745} It is 10-fold selective for p38α over p38β MAPK and 2,000-fold selective over a panel of 20 additional kinases. SCIO 469 inhibits secretion of IL-6 from multiple myeloma patient-derived bone marrow stromal cells (BMSCs) in a concentration-dependent manner. It increases growth inhibition, DNA fragmentation, and caspase-8 and PARP cleavage induced by the proteasome inhibitor PS-341 (bortezomib; Item No. 10008822) in MM.1S cells when used at concentrations of 100 and 200 nM. SCIO 469 (150 and 450 mg/kg) reduces microvessel density and tumor load and increases survival in a 5T33MM murine myeloma model.{48746}