BAY 61-3606

SKU: orb1303010

Description

BAY 61-3606 is a potent, selective, and reversible ATP-competitive inhibitor of spleen tyrosine kinase (Syk) with a Ki of 7.5 nM. It is widely used in vitro and in vivo to investigate Syk's role in immunoreceptor signaling, autoimmune disorders, and hematological malignancies, demonstrating high selectivity over related kinases like Src and Lyn.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 732983-37-8
• MW: 390.4
• Purity: 98.94% (May vary between batches)
• Formula: C₂₀H₁₈N₆O₃
• SMILES: N(C=1N2C(C=C(N1)C3=CC(OC)=C(OC)C=C3)=NC=C2)C4=C(C(N)=O)C=CC=N4
• Target: Apoptosis,Syk
• Solubility: DMSO:3.91 mg/mL (10.02 mM)

Bioactivity

• In Vivo:
  Oral administration of BAY 61-3606 to rats significantly suppressed antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuated antigen-induced airway inflammation in rats.
• In Vitro:
  BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF. BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, BAY 61 3606, BAY 613606, BAY 61-3606, Apoptosis, Spleen tyrosine kinase, Syk, Syk inhibitor IV

Compound Identifiers

PubChem CID

10200390