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

Name: CHMFL-BMX-078
Brand: MedChemExpress
SKU: HY-101267
Rating: 5.0 (1 reviews)

Cat. No.: HY-101267 Purity: ≥98.0%: FAQs
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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.

CHMFL-BMX-078 Chemical Structure

CAS No. : 1808288-51-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 262	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 262	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE CHMFL-BMX-078

•Blood Adv. 2022 Jul 7;bloodadvances.2022007952. [Abstract]

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Biological Activity
Protocol
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References
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Description

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]

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]

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 K_d of 81 nM, while for the active state of BMX kinase, it exhibits a binding K_d 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.

In Vivo

CHMFL-BMX-078 exhibits a short half-life (T_1/2=0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable C_max (13565.23 ng/mL) and AUC_0-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].

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

Molecular Weight

625.67

Formula

C₃₃H₃₅N₇O₆

CAS No.

1808288-51-8

Appearance

Solid

Color

Off-white to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (245 KB) HNMR (214 KB)

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]

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.
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

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

CHMFL-BMX-078 Related Classifications

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.

Keywords:

CHMFL-BMX-0781808288-51-8CHMFL-BMX 078BMX KinaseInhibitorinhibitorinhibit

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

Customer Review

CHMFL-BMX-078 Related Antibodies

1 Publications Citing Use of MCE CHMFL-BMX-078

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CHMFL-BMX-078 Related Antibodies

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Complete Stock Solution Preparation Table

CHMFL-BMX-078 Related Classifications

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