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Product Description
– BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki 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].
Web ID
– HY-76474
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C20H18N6O3
Citations
– Harvard Medical School LINCS LIBRARY|Int J Mol Sci. 2021, 22(7), 3323.|Front Immunol. 2018 Feb 15;9:249.|Neuro Oncol. 2018 Apr 9;20(5):621-631.|Proc Natl Acad Sci U S A. 2022 Oct 25;119(43):e2207280119.
References
– [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. 2003 Sep;306(3):1174-81.|[2]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.|[3]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.|[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.
CAS Number
– 732983-37-8
Molecular Weight
– 390.40
Compound Purity
– 98.21
SMILES
– O=C(C1=CC=CN=C1NC2=NC(C3=CC=C(OC)C(OC)=C3)=CC4=NC=CN24)N
Clinical Information
– No Development Reported
Research Area
– Cancer; Inflammation/Immunology
Solubility
– DMSO : 5 mg/mL (ultrasonic;warming;heat to 80°C)
Target
– Apoptosis;Syk
Pathway
– Apoptosis;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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