BAY 61-3606

SKU: orb1224116

Description

A potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase with Ki of 7.5 nM, displays no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src; inhibits not only degranulation (IC50=5-46 nM) but also lipid mediator and cytokine synthesis in mast cells; suppresses B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes; suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg in rats; orally bioavailable.Allergy Preclinical.

Key Properties

• CAS Number: 732983-37-8
• MW: 390.3953
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₈N₆O₃
• SMILES: O=C(C1=CC=CN=C1NC2=NC(C3=CC=C(OC)C(OC)=C3)=CC4=NC=CN24)N
• Target: Syk
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor. Animal model: Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft. Dosage: 50 mg/kg. Administration: Injected intraperitoneally twice a week with Bay 61-3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks. Result: Led to efficacious reductions in tumor growth.
• In Vitro:
  BAY 61-3606 (0.01-10 μM; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK. BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y. BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation inK-rn cell lysates. Cell Viability Assay Cell line: SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells. Concentration: 0.01, 0.1, 1, and 10 μM Incubation time: 48 hours. Result: Significantly reduced the cell viability of both cell lines in a dose-dependent matter. Western blot analysis. Cell line: SH-SY5Y cells. Concentration: 0.4 and 0.8 μM Incubation time: 4 or 24 hours. Result: Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment. Western blot analysis. Cell line: K-rn cell lysates. Concentration: 2 μM. Incubation time: 2 hours. Result: Induced a large decrease of Syk phosphorylation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAY61-3606

Quick Database Links

Gene Symbol

Syk