Tegatrabetan|BC-2059|CAS 1227637-23-1

Cas No.:	1227637-23-1
Chemical Name:	9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, 9,10-dioxime, rel-
Synonyms:	BC-2059;BC2059;Tegavivint
SMILES:	O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[C@H](C)C[C@H](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[C@H](C)C[C@H](C)C5)=O
Formula:	C₂₈H₃₆N₄O₆S₂
M.Wt:	588.74
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].
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[1]. Animal Model: NOD/SCID mice bearing OCI-AML3 xenografts[1] 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.
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[1]. 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[1]. 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[1]. Cell Proliferation Assay[1] Cell Line: HL-60, OCI-AML3 and MV4-11 cells Concentration: 20, 50, and 100 nM Incubation Time: 48 hours Result: Dose-dependently inhibited cell proliferation. Cell Cycle Analysis[1] Cell Line: OCI-AML3 cells Concentration: 20 and 50 nM Incubation Time: 24 hours Result: Dose-dependently induced cell cycle growth arrest. Western Blot Analysis[1] Cell Line: OCI-AML3, HL-60 and MV4-11 cells Concentration: 100 nM Incubation Time: 24 hours Result: Treatment depleted β-Catenin expression levels.

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