常用名 | Syk抑制剂IV,BAY 61-3606 HCl | CAS号 | 732983-37-8 |
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价格 | ¥需询单/1g ¥需询单/1mg | 纯度 | 98.0% |
备货期 | 需询单 | 库存 | 询单 |
产品详情(用途,包装等)
用途: 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: Sykin 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 [1]. 物理化学性质: CAS号:732983-37-8 常用中文名:Syk抑制剂IV,BAY 61-3606 HCl 常用英文名:BAY 61-3606 分子式:C20H18N6O3 分子量:390.395 密度:1.4±0.1 g/cm3 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:2-8℃ |