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%
COA 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 ¥2753
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1 mg ¥800
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5 mg ¥2000
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10 mg ¥3200
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25 mg ¥5440
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Customer Review

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]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
5637 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 5637 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 5637 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
769-P GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 769-P cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 769-P cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
A498 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human A498 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human A498 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
ACHN GI50
4.93 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human ACHN cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human ACHN cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
BaF3 GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
CHO GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
CWR22R GI50
3.45 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human 22Rv1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human 22Rv1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
DU-145 GI50
7.89 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human DU145 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human DU145 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
EJ GI50
> 10 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human EJ cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human EJ cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
J82 GI50
5.78 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human J82 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human J82 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
PC-3 GI50
3.45 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human PC3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human PC3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
T-24 GI50
8.98 μM
Compound: 41; CHMFL-BMX-078
Growth inhibition of human T24 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
Growth inhibition of human T24 cells after 72 hrs by CellTiter-Glo or CCK-8 assay
[PMID: 28140585]
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
性状

固体

颜色

Off-white to yellow

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 30 mg/mL (47.95 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    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); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.00 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

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

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5983 mL 7.9914 mL 15.9829 mL 39.9572 mL
5 mM 0.3197 mL 1.5983 mL 3.1966 mL 7.9914 mL
10 mM 0.1598 mL 0.7991 mL 1.5983 mL 3.9957 mL
15 mM 0.1066 mL 0.5328 mL 1.0655 mL 2.6638 mL
20 mM 0.0799 mL 0.3996 mL 0.7991 mL 1.9979 mL
25 mM 0.0639 mL 0.3197 mL 0.6393 mL 1.5983 mL
30 mM 0.0533 mL 0.2664 mL 0.5328 mL 1.3319 mL
40 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9989 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CHMFL-BMX-078
目录号:
HY-101267
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