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Tegatrabetan

CAS No. : 1227637-23-1

MCE 站：Tegatrabetan

产品活性：Tegatrabetan (BC2059) 是一种 β-Catenin 拮抗剂。Tegatrabetan 破坏 β-catenin 与转导素 β 样蛋白 1 (TBL1) 结合。

研究领域：Stem Cell/Wnt

作用靶点：β-catenin

In Vitro: Tegatrabetan (BC2059; 20-100 nM; 48 hours) inhibits cell proliferation in suspension culture over 120 hours and induces apoptosis of cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3 and MV4-11 cells dose-dependently.
Tegatrabetan (20 and 50 nM; 24 hours) induces a modest but significant accumulation of cells in the G0/G1 phase, with a concomitant decline in the G2/M phase of the cell cycle.
Tegatrabetan (100 nM, 24 hours) depletes the levels of β-catenin and its target genes, including c-MYC and survivin without affecting the levels of the TBL1 in OCI-AML3, HL-60 and MV4-11 cells.

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.

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