1227637-23-1
1227637-23-1 structure
- Name: BC2059
- Chemical Name: 2,7-Bis{[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl}-N,N'-dihydroxy-9,10-anthracenediimine
- CAS Number: 1227637-23-1
- Molecular Formula: C28H36N4O6S2
- Molecular Weight: 588.739
- Catalog: Research Areas Cancer
- Create Date: 2018-06-24 20:43:11
- Modify Date: 2024-01-06 11:16:41
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Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].
| Name | 2,7-Bis{[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl}-N,N'-dihydroxy-9,10-anthracenediimine |
|---|---|
| Synonyms |
2,7-Bis{[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl}-N,N'-dihydroxy-9,10-anthracenediimine
9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, dioxime BC2059 |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
β-Catenin[1] |
| 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. |
| 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. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 757.6±70.0 °C at 760 mmHg |
| Molecular Formula | C28H36N4O6S2 |
| Molecular Weight | 588.739 |
| Flash Point | 412.0±35.7 °C |
| Exact Mass | 588.207642 |
| LogP | 4.86 |
| Vapour Pressure | 0.0±2.7 mmHg at 25°C |
| Index of Refraction | 1.687 |