Galicaftor (ABBV-2222)

For research use only.

Catalog No.S8535 Synonyms: GLPG2222

Galicaftor (ABBV-2222) Chemical Structure

CAS No. 1918143-53-9

Galicaftor (ABBV-2222, GLPG2222) is a potent corrector of CFTR for the treatment of Cystic Fibrosis (CF).

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Biological Activity

Description Galicaftor (ABBV-2222, GLPG2222) is a potent corrector of CFTR for the treatment of Cystic Fibrosis (CF).
Targets
CFTR [1]
()
In vitro

ABBV-2222/GLPG2222 exhibits potent in vitro functional activity in primary patient cells harboring F508del/F508del CFTR with an EC50 <10 nM. ABBV-2222 promotes maturation of F508delCFTR, and stabilizes nucleotide binding domain 1 - membrane spanning domain interface. ABBV-2222 corrects F508delCFTR through action on membrane spanning domain 1.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: CFBE41o-F508del CFTR-HRP cells
  • Concentrations: 0 - 20 μM
  • Incubation Time: 18-24 h
  • Method:

    the CFBE41o-F508del CFTR-HRP cells are plated in 384-well plates at 4,000 cells/well along with 0.5 μg/mL doxycycline to induce the F508del CFTR-HRP expression and further incubated at 37 oC, 5% CO2 for 72 hours. ABBV-2222/GLPG2222 is then added at the required concentrations and further incubated for 18-24 hours at 33 °C. The highest concentration tested is 20 μM with an 8-12 point concentration response curve using a 3-fold dilution.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (178.74 mM)
Water Insoluble
Ethanol '100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 559.46
Formula

C28H21F4NO7

CAS No. 1918143-53-9
Storage powder
in solvent
Synonyms GLPG2222
Smiles C1CC1(C2=CC3=C(C=C2)OC(O3)(F)F)C(=O)NC4CC(OC5=C4C=CC(=C5)OC(F)F)C6=CC=C(C=C6)C(=O)O

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CFTR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID