| Bioactivity | 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]. | ||||||||||||
| Invitro | β-catenin-IN-6 (compound 9) (24 h) 对 LoVo 和 HT29 细胞具有抑制作用，IC50 分别为 1.4 μM和 1.37 μM。β-catenin-IN-6 显示出对几种人类结直肠癌细胞系的细胞生长抑制作用[1]。 | ||||||||||||
| In Vivo | β-catenin-IN-6 (compound 9) 的生物利用度较差[1]。β-catenin-IN-6 (18.75 mg/kg；腹腔注射；每日 1 次，共 7 天) 可减少小鼠肿瘤体积，不影响体重[1]。β-catenin-IN-6 (compound 13) (150 mg/kg；腹腔注射；每周 1 次) 抑制 β-catenin/RK3E 小鼠模型中异植肿瘤的生长[2]。 Animal Model: | ||||||||||||
| Name | β-catenin-IN-6 | ||||||||||||
| CAS | 1039731-99-1 | ||||||||||||
| Formula | C22H19ClN6O | ||||||||||||
| Molar Mass | 418.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. [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. |
β-catenin-IN-6
CAS: 1039731-99-1 F: C22H19ClN6O W: 418.88
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway.
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