|
|
| Product Name: | BC2059 | | Synonyms: | BC2059;BC-2059;BC2059;TEGAVIVINT;TEGATRABETAN;BC-2059;TEGAVIVINT;9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, 9,10-dioxime, rel-;rel-2,7-Bis(((3R,5S)-3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime;Tegatrabetan (BC2059);Tegatrabetan,inhibit,Inhibitor,β-catenin,BC-2059,Beta catenin,BC 2059;BC-2059 Te atrabetan | | CAS: | 1227637-23-1 | | MF: | C28H36N4O6S2 | | MW: | 588.74 | | EINECS: | | | Product Categories: | | | Mol File: | 1227637-23-1.mol |  |
| | BC2059 Chemical Properties |
| Melting point | 287 °C(Solvent: Dichloromethane; Hexane) | | Boiling point | 757.6±70.0 °C(Predicted) | | density | 1.46±0.1 g/cm3(Predicted) | | storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | DMSO: 125 mg/mL (212.32 mM) | | pka | 10.07±0.20(Predicted) | | form | Solid | | color | White to light yellow | | InChIKey | LQQUOMJXUXVPRB-IOTKHNBZSA-N | | SMILES | [S](=O)(=O)(N5C[C@H](C[C@H](C5)C)C)c1cc2c(cc1)C(c3c(cc(cc3)[S](=O)(=O)N4C[C@H](C[C@H](C4)C)C)C2N=O)N=O |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | BC2059 Usage And Synthesis |
| 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. | | | target | | | 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 |
| | BC2059 Preparation Products And Raw materials |
|