Uses
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].
Biological Activity
Tegatrabetan (BC2059) is a beta-Catenin antagonist. It disrupts β-catenin binding to scaffold protein transducin β-like 1 (TBL1) and proteasomal degradation and reduces β-catenin nuclear levels.
in vivo
Tegatrabetan (BC2059; 1.0 or 5.0 mg/kg/day; intravenously) significantly improves the median survival of the mice from approximately 17.5 to 39 days. Treatment with Tegatrabetan (10 mg/kg/day; intravenously) alone further improves the median survival to 51.5 days.
| Animal Model: | NOD/SCID mice bearing OCI-AML3 xenografts | < /tr>
| Dosage: | 1 mg/kg; 5 mg/kg; 10 mg/kg |
| Administration: | Intravenously; 1 mg/kg daily 4 days per week or 5 mg/kg or 10 mg/kg of BC2059 twice per week (Tuesday and Thursday) for 3 weeks. |
| Result: | Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts. |
References
[1] Fiskus W, et al. Pre-clinical efficacy of combined therapy with novel β-catenin antagonist BC2059 and histone deacetylase inhibitor against AML cells. Leukemia. 2015 Jun;29(6):1267-78. DOI:
10.1038/leu.2014.340
