CHMFL-BMX-078

SKU: orb1303005

Description

CHMFL-BMX-078 is a potent, irreversible type II inhibitor of BMX kinase, demonstrating high selectivity and an IC50 value of 11 nM. It is a valuable research tool for studying BMX function in oncology and immunology, with utility in both cellular and in vivo models of cancer and inflammatory diseases.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1808288-51-8
• MW: 625.67
• Purity: 98.00% (May vary between batches)
• Formula: C₃₃H₃₅N₇O₆
• SMILES: CNc1nc(Nc2ccc(C)c(NC(=O)C=C)c2)ncc1C(=O)Nc1cc(NC(=O)c2cc(OC)c(OC)c(OC)c2)ccc1C
• Target: BTK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.2 mM);DMSO:30 mg/mL (47.95 mM)

Bioactivity

• Target IC50:
  BMX kinase:11 nM.
• 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.
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• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CHMFL BMX 078, CHMFL-BMX 078, CHMFLBMX078, CHMFL-BMX078, CHMFL-BMX-078, Bmx, BMX Kinase, inhibit, Inhibitor

Compound Identifiers

PubChem CID

122633900