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CHMFL-BMX-078

Catalog No. T4268 CAS 1808288-51-8

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

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CHMFL-BMX-078, CAS 1808288-51-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 80.00
5 mg	In stock	$ 197.00
10 mg	In stock	$ 313.00
25 mg	In stock	$ 590.00
50 mg	In stock	$ 852.00
100 mg	In stock	$ 1,170.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 98%

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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.
Targets&IC50	BMX kinase:11 nM.
In vitro	CHMFL-BMX-078 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.
In vivo	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 i.v. or i.p. injection when used as a research tool.
Kinase Assay	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.
Animal Research	CHMFL-BMX-078 is dissolved in 55% saline containing 5% DMSO and 40% PEG400 by vortex. The final concentration of the stock solution is 1 mg/mL for administration.Rat: 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.

Molecular Weight	625.67
Formula	C33H35N7O6
CAS No.	1808288-51-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (47.95 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Target-Focused Phenotypic Screening Library Kinase Inhibitor Library Angiogenesis related Compound Library Covalent Inhibitor Library NO PAINS Compound Library Cysteine Covalent Library Bioactive Compounds Library Max Bioactive Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

CHMFL-BMX-078 1808288-51-8 Angiogenesis Tyrosine Kinase/Adaptors BTK CHMFLBMX078 BMX Kinase inhibit CHMFL BMX 078 CHMFL-BMX 078 Inhibitor CHMFL-BMX078 inhibitor

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