| Identification | Back Directory | [Name]
3-PyridinecarboxaMide, 6-chloro-N-[4-[[[2-(MethylaMino)-4-quinazolinyl]aMino]Methyl]phenyl]- | [CAS]
1039731-99-1 | [Synonyms]
β-catenin-IN-6
6-Chloro-N-(4-(((2-(methylamino)quinazolin-4-yl)amino)methyl)phenyl)nicotinamide
6-chloro-N-[4-[[[2-(methylamino)quinazolin-4-yl]amino]methyl]phenyl]pyridine-3-carboxamide
3-PyridinecarboxaMide, 6-chloro-N-[4-[[[2-(MethylaMino)-4-quinazolinyl]aMino]Methyl]phenyl]- | [Molecular Formula]
C22H19ClN6O | [MOL File]
1039731-99-1.mol | [Molecular Weight]
418.88 |
| Hazard Information | Back Directory | [Uses]
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model[1][2]. | [in vivo]
β-catenin-IN-6 (compound 9) displays poor bioavailability[1].
β-catenin-IN-6 (18.75 mg/kg; ip; once daily for 7 days) decreases tumor volume in mouse model, without affecting body weight[1].
β-catenin-IN-6 (compound 13) (150 mg/kg; ip; once per week) suppresses xenograft tumor growth in a β-catenin/RK3E mouse model[2].
| Animal Model: | Nude mice bearing subcutaneous β-catenin/ RK3E tumors[1][2] | | Dosage: |
18.75 mg/kg, 37.5 mg/kg, 75.1 mg/kg, 150 mg/kg | | Administration: | IP; once daily for 7 days | | Result: | Inhibited tumor growth up to 66% in mouse model.
Showed dose-dependently inhibition on tumor growth and volume. |
| [References]
[1] Dehnhardt CM, et al. Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition. J Med Chem. 2010 Jan 28;53(2):897-910. DOI:10.1021/jm901370m
[2] McCoy MA, et al. Biophysical Survey of Small-Molecule β-Catenin Inhibitors: A Cautionary Tale. J Med Chem. 2022 May 26;65(10):7246-7261. DOI:10.1021/acs.jmedchem.2c00228 |
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