1227637-23-1
1227637-23-1 性质
| 熔点 | 287 °C(Solvent: Dichloromethane; Hexane) |
|---|---|
| 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 |
| 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 |
1227637-23-1 用途与合成方法
| 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. |
1227637-23-1 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-109103 | 1227637-23-1 | 1227637-23-1 | 1 mg | 681 |
| 2026-09-15 | HY-109103 | 1227637-23-1 | 1227637-23-1 | 5 mg | 1500 |
