BAY 61-3606 dihydrochloride

SKU: orb1300477

Description

BAY 61-3606 dihydrochloride is a highly selective and potent inhibitor of spleen tyrosine kinase (Syk), exhibiting a Ki of 7.5 nM. This compound is widely used in research to investigate Syk's role in immunology and oncology, facilitating both in vitro biochemical assays and in vivo disease model studies.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 648903-57-5
• MW: 463.32
• Purity: 99.46%
• Formula: C₂₀H₁₈N₆O₃·2HCl
• SMILES: Cl.Cl.COc1ccc(cc1OC)-c1cc2nccn2c(Nc2ncccc2C(N)=O)n1
• Target: Apoptosis,Syk
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:0.5 mg/mL (1.08 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:12 mg/mL (25.9 mM)

Bioactivity

• Target IC50:
  Syk:7.5 nM(Ki)
• In Vivo:
  After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats.
• In Vitro:
  BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM.
• Cell Research:
  MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.(Only for Reference)

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

BAY-61-3606, BAY-61-3606 Dihydrochloride, BAY-61-3606 dihydrochloride, BAY 61 3606 dihydrochloride, BAY 61-3606, BAY 613606 dihydrochloride, BAY 61-3606 Dihydrochloride, Apoptosis, Inhibitor, inhibit, Syk, Spleen tyrosine kinase

Compound Identifiers

PubChem CID

11784504