BAY 61-3606 (hydrochloride)

BAY 61-3606 is an inhibitor of spleen tyrosine kinase (Syk, Ki = 7.5 nM). It is selective for Syk over Lyn, Fyn, Src, Itk, and BTK (Kis = >4.7 µM for all). BAY 61-3606 inhibits anti-IgE-induced histamine release in isolated human mast cells sensitized with IgE (IC50 = 5.1 nM), as well as reduces anti-IgM-induced proliferation of isolated mouse splenic B cells (IC50 = 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 (ED50 = 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.Formal Name: 2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide, monohydrochloride. CAS Number: 1615197-10-8. Molecular Formula: C20H18N6O3 . HCl. Formula Weight: 426.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 10 mg/ml. lambdamax: 331 nm. SMILES: NC(C1=C(NC2=NC(C3=CC(OC)=C(OC)C=C3)=CC4=NC=CN24)N=CC=C1)=O.Cl. InChi Code: InChI=1S/C20H18N6O3.ClH/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19,/h3-11H,1-2H3,(H2,21,27)(H,23,24,25),1H. InChi Key: HLYFDKZWVIBYKL-UHFFFAOYSA-N.