1. Protein Tyrosine Kinase/RTK
  2. BMX Kinase
  3. CHMFL-BMX-078

CHMFL-BMX-078 (Synonyms: CHMFL-BMX 078)

目录号: HY-101267 纯度: ≥98.0%
产品使用指南

CHMFL-BMX-078是高效的,选择性的,不可逆的,类型II BMX激酶抑制剂,IC50值为11 nM。

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CHMFL-BMX-078 Chemical Structure

CHMFL-BMX-078 Chemical Structure

CAS No. : 1808288-51-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4818
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1 mg ¥1200
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5 mg ¥3500
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10 mg ¥5500
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50 mg ¥16500
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100 mg ¥22500
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.

IC50 & Target

IC50: 11 nM (BMX)[1]

体外研究
(In Vitro)

Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC50=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding Kd of 81 nM, while for the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI50=0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC50=5.8 nM) than C496S mutant (EC50=459 nM) for the inhibition of BMX total tyrosine phosphorylation. CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CHMFL-BMX-078 exhibits a short half-life (T1/2=0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable Cmax (13565.23 ng/mL) and AUC0-t (1386.41 ng/mL h) in iv injection. However, it is not absorbed by oral administration, indicating that this compound could be administrated through iv or ip injection when used as a research tool[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

625.67

Formula

C33H35N7O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 30 mg/mL (47.95 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5983 mL 7.9914 mL 15.9829 mL
5 mM 0.3197 mL 1.5983 mL 3.1966 mL
10 mM 0.1598 mL 0.7991 mL 1.5983 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.00 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.00 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Kinase Assay
[1]

The kinase reaction system contains BMX or BTK, 1 μL of serially diluted CHMFL-BMX-078, and substrate Poly peptidewith 100 μM ATP. The reaction in each tube is started immediately by adding ATP and kept going for an hour under 37 °C. After the tube cooled for 5 min at room temperature, 5 μL solvent reactions are carried out in a 384-well plate. Then 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ATP within 40 min. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 30 min to produce a luminescence signal. Luminescence signal is measured with an automated plate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats: Six 8-week-old male Sprague−Dawley rats are fasted overnight before starting drug treatment via intravenous and oral administration. Animal blood collection time points are as follows. For groups 1, 3, and 5 (intravenous): 1 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h before and after administration is selected. For group 2, 4, and 6 (oral): 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h before and after dosing. The plasma is collected for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

纯度: ≥98.0%

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产品名称:
CHMFL-BMX-078
目录号:
HY-101267
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