1227637-23-1
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- CAS号:
- 1227637-23-1
- 英文名:
- BC2059
- 英文别名:
- BC2059;Tegavivint;Tegoprazan D6;Tegatrabetan (BC2059);BC-2059;BC2059;TEGAVIVINT;TEGATRABETAN;BC-2059;TEGAVIVINT;Tegatrabetan,inhibit,Inhibitor,β-catenin,BC-2059,Beta catenin,BC 2059;rel-2,7-Bis(((3R,5S)-3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime;9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, 9,10-dioxime, rel-
- 中文名:
- 1227637-23-1
- 中文别名:
- 化合物BC2059;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
- CBNumber:
- CB03038499
- 分子式:
- C28H36N4O6S2
- 分子量:
- 588.74
- MOL File:
- 1227637-23-1.mol
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1227637-23-1化学性质
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沸点:
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757.6±70.0 °C(Predicted)
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密度:
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1.46±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2-8°C
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溶解度:
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DMSO: 125 mg/mL (212.32 mM)
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酸度系数(pKa):
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10.07±0.20(Predicted)
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形态:
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Solid
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颜色:
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White to light yellow
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1227637-23-1性质、用途与生产工艺
Tegatrabetan (BC2059) 是一种 β-Catenin 的拮抗剂。Tegatrabetan (BC2059) 会破坏β-catenin与scaffold protein transducin β-like 1 (TBL1)的结合以及蛋白酶体降解并降低β-catenin核水平。
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
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Cell Line:
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HL-60, OCI-AML3 and MV4-11 cells
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Concentration:
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20, 50, and 100 nM
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Incubation Time:
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48 hours
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Result:
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Dose-dependently inhibited cell proliferation.
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Cell Cycle Analysis
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Cell Line:
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OCI-AML3 cells
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Concentration:
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20 and 50 nM
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Incubation Time:
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24 hours
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Result:
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Dose-dependently induced cell cycle growth arrest.
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Western Blot Analysis
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Cell Line:
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OCI-AML3, HL-60 and MV4-11 cells
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Concentration:
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100 nM
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Incubation Time:
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24 hours
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Result:
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Treatment depleted β-Catenin expression levels.
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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.
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Animal Model:
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NOD/SCID mice bearing OCI-AML3 xenografts
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Dosage:
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1 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:
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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.
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Result:
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Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
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1227637-23-1
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
1227637-23-1, 1227637-23-1 相关搜索:
- 药靶配体
- 对照品
- 化合物BC2059
- 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
- 1227637-23-1
- Tegoprazan D6
- Tegatrabetan,inhibit,Inhibitor,β-catenin,BC-2059,Beta catenin,BC 2059
- Tegatrabetan (BC2059)
- rel-2,7-Bis(((3R,5S)-3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime
- 9,10-Anthracenedione, 2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-, 9,10-dioxime, rel-
- TEGATRABETAN;BC-2059;TEGAVIVINT
- Tegavivint
- BC-2059;BC2059;TEGAVIVINT
- BC2059