BAY 61-3606 

BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i of 7.5 nM and an IC₅₀ of 10 nM^[1]. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell^[2]. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates^[3]. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells^[4].

Ki: 7.5 nM (Syk)^[1]
IC50: 10 nM (Syk)^[1]

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^[2].
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^[2].
BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

390.40

C₂₀H₁₈N₆O₃

732983-37-8

Solid

Light yellow to yellow

O=C(C1=CC=CN=C1NC2=NC(C3=CC=C(OC)C(OC)=C3)=CC4=NC=CN24)N

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Yamamoto N, et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2  [Content Brief]

  [2]. Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to nilotinib in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21.  [Content Brief]

  [3]. Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202.  [Content Brief]

  [4]. Kim SY, et al. Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells. PLoS One. 2015 Dec 31;10(12):e0146073.  [Content Brief]