1227637-23-1
- CAS号:1227637-23-1
- 英文名:BC2059
- 中文名:1227637-23-1
- CBNumber:CB03038499
- 分子式:C28H36N4O6S2
- 分子量:588.74
- MOL File:1227637-23-1.mol
- 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 :DMSO: 125 mg/mL (212.32 mM)
- 酸度系数(pKa) :10.07±0.20(Predicted)
- 形态 :Solid
- 颜色 :White to light yellow
1227637-23-1性质、用途与生产工艺
- 生物活性 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。
-
靶点
Target Value β-catenin
() -
体外研究
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. -
体内研究
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.
- 更新日期：2024/11/08
- 产品编号：S0733
- 产品名称：1227637-23-1 Tegatrabetan (BC-2059)
- CAS编号：1227637-23-1
- 包装：5mg
- 价格：2269.4元
- 更新日期：2024/11/08
- 产品编号：S0733
- 产品名称：Tegatrabetan (BC-2059)
- CAS编号：1227637-23-1
- 包装：10mM (1mL in DMSO)
- 价格：2694.51元
- 公司名称：AdooQ BioScience, LLC
- 联系电话：+1 (866) 930-6790
- 电子邮件：info@adooq.com
- 国家：美国
- 产品数：2782
- 优势度：58
- 公司名称：InvivoChem
- 联系电话：+1-708-310-1919 +1-13798911105
- 电子邮件：sales@invivochem.cn
- 国家：美国
- 产品数：6391
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57505
- 优势度：58
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：
- 电子邮件：support@targetmol.com
- 国家：美国
- 产品数：38631
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
