化合物BAY 61-3606 T4263

Product Introduction
Bioactivity


英文名: BAY 61-3606

描述: BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的，ATP 竞争性的可逆选择性Syk 抑制剂。它作用于乳腺癌细胞，通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化，也降低 K-rn 细胞裂解物中 Syk 磷酸化。

体外活性: 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. 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.

体内活性: 经口给予大鼠BAY 61-3606，显著抑制了抗原诱导的被动皮肤过敏反应、支气管收缩和支气管水肿，剂量为3 mg/kg。此外，BAY 61-3606还减轻了抗原诱导的大鼠气道炎症。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.9 mg/mL (10 mM)


关键字: Spleen tyrosine kinase | Syk | inhibit | BAY 61 3606 | Apoptosis | BAY 61-3606 | Inhibitor | BAY 613606

相关产品: Salermide | CA-5f | Niraparib | Phytohemagglutinin | Girinimbine | Methotrexate | Pseudolaric Acid B | W-7 hydrochloride | Ro-3306 | B-AP15

相关库: Angiogenesis related Compound Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Orally Active Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途