CHMFL-BMX-078

SKU: orb1303005

Description

CHMFL-BMX-078

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1808288-51-8
• MW: 625.67
• Purity: 100.00%
• 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.
• In Vitro:
  CHMFL-BMX-078 displays a high selectivity profile agains 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 fo the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits ant Proliferative effects against BaF3-TEL-BMX cells (GI5 = .016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC5 = .8 nM) than C496S mutant (EC5 = 59 nM) fo the Inhibition of BMX total tyrosine phosphorylation.
• Animal Research:
  CHMFL-BMX-078 is dissolved in 55% saline containing 5% DMSO and 40% PEG400 by vortex the final concentration o 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• 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