CHMFL-BMX-078
Based on 3 publication(s) in Google Scholar
CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1808288-51-8
- Formula: C33H35N7O6
- Molecular Weight:625.67
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CHMFL-BMX-078
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Biological Activity
IC50: 11 nM (BMX)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 5637 | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| 769-P | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| A498 | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| ACHN | GI50 |
4.93 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| BaF3 | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| CHO | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| CWR22R | GI50 |
3.45 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| DU-145 | GI50 |
7.89 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| EJ | GI50 |
>10 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| J82 | GI50 |
5.78 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| PC-3 | GI50 |
3.45 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
| T-24 | GI50 |
8.98 μM
Compound: 41; CHMFL-BMX-078
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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
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[PMID: 28140585] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1808288-51-8
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Appearance Solid
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Molecular Weight 625.67
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Formula C33H35N7O6
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Color Off-white to yellow
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SMILES
O=C(C1=CN=C(NC2=CC=C(C)C(NC(C=C)=O)=C2)N=C1NC)NC3=CC(NC(C4=CC(OC)=C(OC)C(OC)=C4)=O)=CC=C3C
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Synonyms
CHMFL-BMX 078
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
Bruton tyrosine kinase (Btk) in neutrophils is indispensable for initiating and maintaining skin inflammation in a model of pemphigoid diseases. [Abstract]2026 Jan 18. PMID: 41549045 -
Blood Adv
BMX kinase mediates gilteritinib resistance in FLT3-mutated AML through microenvironmental factors. [Abstract]2022 Sep 13;6(17):5049-5060. PMID: 35797240 -
Solvent & Solubility
DMSO : ≥ 30 mg/mL (47.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Liang X, et al. Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor. J Med Chem. 2017 Mar 9;60(5):1793-1816. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 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 |
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