Tegatrabetan (BC2059) 是一种β-Catenin拮抗剂。Tegatrabetan 破坏 β-catenin 与转导素 β 样蛋白 1 (TBL1) 结合。
| 生物活性 | Tegatrabetan (BC2059) is aβ-Cateninantagonist. Tegatrabetan disrupts the binding ofβ-cateninwith the scaffold protein transducin β-like 1 (TBL1)[1]. |
| IC50& Target | |
体外研究
(In Vitro) | 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[1].
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[1].
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[1].
Cell Proliferation Assay[1] | 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[1] | 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[1] | Cell Line: | OCI-AML3, HL-60 and MV4-11 cells | | Concentration: | 100 nM | | Incubation Time: | 24 hours | | Result: | Treatment depleted β-Catenin expression levels. |
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体内研究
(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[1].
| Animal Model: | NOD/SCID mice bearing OCI-AML3 xenografts[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(84.93 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.6985 mL | 8.4927 mL | 16.9854 mL | | 5 mM | 0.3397 mL | 1.6985 mL | 3.3971 mL | | 10 mM | 0.1699 mL | 0.8493 mL | 1.6985 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.25 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (4.25 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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