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BMX-IN-1 Sale

(Synonyms: N-[2-甲基-5-[9-[4-[(甲基磺酰基)氨基]苯基]-2-氧代苯并[H]-1,6-萘啶-1(2H)-基]苯基]-2-丙烯酰胺,BMX kinase inhibitor) 目录号 : GC11063

A selective BMX and BTK inhibitor

BMX-IN-1 Chemical Structure

Cas No.:1431525-23-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,764.00
现货
2mg
¥810.00
现货
5mg
¥1,530.00
现货
10mg
¥2,700.00
现货
50mg
¥6,750.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Kinase assay

The serially diluted BMX-IN-1 was added to the BTK kinase. After 30 min incubation at RT, ATP (final concentration: 20μM) was added and incubated for 20 min at 37°C. The reactions were stopped by addition of 5X sample buffer. Then the phosphorylation of BTK was detected by western-blot using a pBTK Y551 antibody (BD).

Cell experiment [1]:

Cell lines

Ramos cell line

Preparation method

The solubility of this compound in DMSO is >5.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.3, 1, 3 and 10 uM for 16/24/48 hours.

Applications

In Ramos cell line, BMX-IN-1 significantly inhibited cell cycle progression at G0/G1 in a dose-dependent manner at 24h and strongly induced apoptosis at a concentration of 1 μM at 8h, while with a longer drug exposure (24 hours), a concentration of 300 nM was sufficient to induce apoptosis.

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.

产品描述

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

Cas No. 1431525-23-3 SDF
别名 N-[2-甲基-5-[9-[4-[(甲基磺酰基)氨基]苯基]-2-氧代苯并[H]-1,6-萘啶-1(2H)-基]苯基]-2-丙烯酰胺,BMX kinase inhibitor
化学名 N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide
Canonical SMILES CC1=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
分子式 C29H24N4O4S 分子量 524.59
溶解度 ≥ 5.25 mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9063 mL 9.5313 mL 19.0625 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL
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