1039731-99-1

Name	3-PyridinecarboxaMide, 6-chloro-N-[4-[[[2-(MethylaMino)-4-quinazolinyl]aMino]Methyl]phenyl]-
CAS	1039731-99-1
Molecular Formula	C22H19ClN6O
Molecular Weight	418.88
MOL File	1039731-99-1.mol

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]-

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Chemical Properties

density	1.426±0.06 g/cm3(Predicted)
form	Solid
pka	11.44±0.70(Predicted)
color	White to off-white

Hazard Information

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

Supplier

Zhejiang J&C Biological Technology Co.,Limited

Telephone+1-2135480471 +1-2135480471;

Websitehttps://www.sarms4muscle.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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