BAY-61-3606

Chemical Information
Product Name BAY-61-3606 CAS No. 732983-37-8
Molecular Weight 463.32 Molecular Formula C20H20Cl2N6O3
MOQ 10g Brand Biolang

Product Description

BAY 61-3606 is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. IC50 value: 7.5 nM (Ki) [1] Target: Syk in vitro: 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 [1]. We identified 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 [2]. 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.

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About Biolang

Shanghai Biolang Bio-Tech Co., Ltd., founded in 2004, located in Shanghai and Nanjing, R&D and logistics center located in Wuhan National Bioindustry Base,the production base in Luotian, Tongshan, Dongying, Pingxiang.Biolang is specialized manufacturer and supplier of New-Type pharmaceutical Raw Materials and Pharmaceutical Intermediates.