BAY 61-3606 is an inhibitor of spleen tyrosine kinase (Syk; K = 7.5 nM). It is selective for Syk over Lyn, Fyn, Src, Itk, and BTK (Ks = >4.7 µM for all). BAY 61-3606 inhibits anti-IgE-induced histamine release in isolated human mast cells sensitized with IgE (IC = 5.1 nM), as well as reduces anti-IgM-induced proliferation of isolated mouse splenic B cells (IC = 58 nM). It sensitizes MCF-7 human breast cancer cells to apoptosis induced by TNF-related apoptosis-inducing ligand (TRAIL) when used at concentrations ranging from 0.31 to 2.5 µM. BAY 61-3606 inhibits passive cutaneous anaphylaxis in rats (ED = 8 mg/kg). It reduces tumor growth in an MCF-7 mouse xenograft model when administered at a dose of 50 mg/kg alone or in combination with TRAIL.
BAY 61-3606 (hydrochloride) is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 (hydrochloride) reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 (hydrochloride) induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 (hydrochloride) sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
分子式
C20H18N6O3.HCl
分子量
426.86
CAS号
1615197-10-8
中文名称
BAY 61-3606 (hydrochloride)
运输条件
Room temperature in continental US; may vary elsewhere.