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BAY 61-3606 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY 61-3606 dihydrochloride图片
CAS NO:648903-57-5
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
BAY-61-3606 dihydrochloride
BAY 61-3606
产品介绍
BAY 61-3606 dihydrochloride 是一种口服有效的,ATP 竞争性的,可逆的选择性Syk抑制剂。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。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。

产品描述

BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

体外活性

BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling[1]. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM[2].

体内活性

After 20 days of drug administration, the volume of the xenografted tumor was significantly (P<0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination[2]. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats[1].

激酶实验

GST-Syk (3.2?ng), 0.5?μg AL, 30?μM ATP, and testing compound in the presence of 0.25% Me2SO are mixed in 50?μL/well of kinase assay buffer in polypropylene U-bottom 96-well microtiter plates. The mixture is incubated for 1?h at room temperature, and the reaction is terminated by the addition of 120?μL of termination buffer. To capture AL, 120?μL of the terminated mixture is transferred to streptavidin-coated plates, followed by incubation at room temperature for more than 30?min. After three ishes with washing buffer, 100?μL of antibody buffer is added and incubated at room temperature for more than 30?min. After three more ishes, 100?μL of enhancement solution is added. Time-resolved fluorescence is measured by multilabel counter ARVO.

细胞实验

MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.(Only for Reference)

Cas No.

648903-57-5

分子式

C20H20Cl2N6O3

分子量

463.32

别名

BAY-61-3606 dihydrochloride;BAY 61-3606

储存和溶解度

H2O:<1 mgml
DMSO:12 mg/mL (25.9 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years