1227637-23-1
| 中文名称 | 1227637-23-1 |
|---|---|
| 中文同义词 | REL-2,7-双(((3R,5S)-3,5-二甲基哌啶-1-基)磺酰基)蒽-9,10-二酮二肟;化合物BC2059 |
| 英文名称 | BC2059 |
| 英文同义词 | BC2059;BC-2059;BC2059;TEGAVIVINT;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 |
| CAS号 | 1227637-23-1 |
| 分子式 | C28H36N4O6S2 |
| 分子量 | 588.74 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | 1227637-23-1.mol |
| 结构式 |  |
1227637-23-1 性质
| 沸点 | 757.6±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.46±0.1 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 溶解度 | 二甲基亚砜：125 mg/mL（212.32 mM） |
| 酸度系数(pKa) | 10.07±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至浅黄色 |
| Target | Value |
|
β-catenin
() |
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.
Cell Proliferation Assay
| 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
| 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
| Cell Line: | OCI-AML3, HL-60 and MV4-11 cells |
| Concentration: | 100 nM |
| Incubation Time: | 24 hours |
| Result: | Treatment depleted β-Catenin expression levels. |
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 |
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | S0733 | 1227637-23-1 Tegatrabetan (BC-2059) | 1227637-23-1 | 5mg | 2269.4元 |
| 2024/04/30 | S0733 | Tegatrabetan (BC-2059) | 1227637-23-1 | 10mM (1mL in DMSO) | 2694.51元 |