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CHMFL-BMX-078

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Catalog No. T4268Cas No. 1808288-51-8

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

CHMFL-BMX-078

CHMFL-BMX-078

🥰Excellent
Purity: 100%
Catalog No. T4268Cas No. 1808288-51-8
CHMFL-BMX-078 is a highly potent and selective type II irreversible inhibitor of BMX kinase, with an IC50 of 11 nM.
Pack SizePriceAvailabilityQuantity
1 mg$64In Stock
5 mg$156In Stock
10 mg$247In Stock
25 mg$446In Stock
50 mg$619In Stock
100 mg$859In Stock
1 mL x 10 mM (in DMSO)$215In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
CHMFL-BMX-078 is a highly potent and selective type II irreversible inhibitor of BMX kinase, 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.
Chemical Properties
Molecular Weight625.67
FormulaC33H35N7O6
Cas No.1808288-51-8
SmilesCNc1nc(Nc2ccc(C)c(NC(=O)C=C)c2)ncc1C(=O)Nc1cc(NC(=O)c2cc(OC)c(OC)c(OC)c2)ccc1C
Relative Density.1.335 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 30 mg/mL (47.95 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5983 mL7.9914 mL15.9829 mL79.9143 mL
5 mM0.3197 mL1.5983 mL3.1966 mL15.9829 mL
10 mM0.1598 mL0.7991 mL1.5983 mL7.9914 mL
20 mM0.0799 mL0.3996 mL0.7991 mL3.9957 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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