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BMX-IN-1

现货
Catalog No.
A3260
BMX(又称ETK)激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 3,250.00
Ship with 10-15 days
2mg
¥ 950.00
现货
5mg
¥ 1,700.00
Ship with 10-15 days
10mg
¥ 3,000.00
Ship with 10-15 days
50mg
¥ 9,900.00
Ship with 10-15 days
100mg
¥ 14,000.00
Ship with 10-15 days

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Background

BMX-IN-1 is a highly selective and irreversible inhibitor of BMX kinase [1].
BMX, also known as ETK, is a member of Tec family and plays an important role in regulating ischemia-mediated arteriogenesis and lymphangiogenesis. BMX is mainly expressed in arterial endothelia and in myeloid hematopoietic cells and it has been reported that BMX involves in tumor growth [2].
BMX-IN-1 is a potent BMX kinase inhibitor and has an irreversible function on BMX kinase. When tested with prostate cancer cell lines, BMX-IN-1 treatment inhibited the proliferation of Tel-BMX-transformed Ba/F3 cells at lowdose [1].
References:
[1].Liu, F., et al., Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol, 2013. 8(7): p. 1423-8.
[2].Holopainen, T., et al., Deletion of the endothelial Bmx tyrosine kinase decreases tumor angiogenesis and growth. Cancer Res, 2012. 72(14): p. 3512-21.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt524.59
Cas No.1431525-23-3
FormulaC29H24N4O4S
SynonymsBMX kinase inhibitor
Solubility≥5.25 mg/mL in DMSO, <2.35 mg/mL in EtOH, <2.16 mg/mL in H2O
Chemical NameN-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide
SDFDownload SDF
Canonical SMILESCC1=C(C=C(C=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CC=C(C=C5)NS(=O)(=O)C)NC(=O)C=C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

酶学实验 [1]:

激酶检测

将连续稀释的BMX-IN-1加入到BTK激酶中。在室温下30分钟温育后,加入ATP(终浓度:20μM),并在37℃下孵育20分钟。加入5X样品缓冲液停止反应。使用pBTK Y551抗体通过western印迹检测BTK的磷酸化。

细胞实验 [1]:

细胞系

Ramos细胞系

溶解方法

在DMSO中的溶解度>5.3 mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0.3,1,3和10 uM,孵育16、24、48小时

应用

在Ramos细胞系中,BMX-IN-1在24h时以剂量依赖性方式显著抑制G0/G1期的细胞周期进程,8h时浓度为1μM时,强烈诱导细胞凋亡,药物暴露时间增加到24小时时,300nM的浓度足以诱导细胞凋亡。

References:

[1]. Hong Wu, et al. Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol. 2014 May 16; 9(5): 1086–1091.

生物活性

Description BMX-IN-1是一种高选择性的和强效的不可逆BMX激酶抑制剂。
靶点 BMX Kinase          
IC50            

质量控制

化学结构

BMX-IN-1