Tegatrabetan Tegavivint; BC2059|cas:1227637-23-1|西域试剂

Tegatrabetan Tegavivint; BC2059,99.77%

产品编号：Bellancom-109103| CAS NO：1227637-23-1| 分子式：C₂₈H₃₆N₄O₆S₂| 分子量：588.74

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货号	价格	库存与货期
Bellancom-109103	￥2700.00	杭州北京（现货）
Bellancom-109103	￥4500.00	杭州北京（现货）
Bellancom-109103	￥11500.00	杭州北京（现货）
Bellancom-109103	￥0.00	杭州北京（现货）

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Tegatrabetan Tegavivint; BC2059

产品介绍

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 a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (84.93 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。