2. Stem Cell/Wnt
  3. β-catenin
  4. Tegatrabetan

Tegatrabetan  (Synonyms: Tegavivint; BC2059)

目录号: HY-109103 纯度: 99.77%
COA 产品使用指南

摩尔计算器

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。

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Tegatrabetan Chemical Structure

Tegatrabetan Chemical Structure

CAS No. : 1227637-23-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1943
In-stock
1 mg ￥681
In-stock
5 mg ￥1500
In-stock
10 mg ￥2450
In-stock
25 mg ￥4273
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Tegatrabetan 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

IC50 & Target

β-Catenin[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.05169 μM
Compound: 14, BC-2059
Growth inhibition of human A549 cells after 72 hrs by APH assay
Growth inhibition of human A549 cells after 72 hrs by APH assay
[PMID: 26182238]
Cancer cell lines IC50
0.02001 μM
Compound: 14, BC-2059
Cytotoxicity against human breast cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
Cytotoxicity against human breast cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
[PMID: 26182238]
Cancer cell lines IC50
0.02075 μM
Compound: 14, BC-2059
Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay
Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay
[PMID: 26182238]
Cancer cell lines IC50
0.02992 μM
Compound: 14, BC-2059
Cytotoxicity against human colon cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
Cytotoxicity against human colon cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
[PMID: 26182238]
Cancer cell lines IC50
0.5305 μM
Compound: 14, BC-2059
Cytotoxicity against human ovarian cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
Cytotoxicity against human ovarian cancer cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
[PMID: 26182238]
HCT-116 IC50
0.02019 μM
Compound: 14, BC-2059
Growth inhibition of human HCT116 cells after 72 hrs by APH assay
Growth inhibition of human HCT116 cells after 72 hrs by APH assay
[PMID: 26182238]
HCT-15 IC50
0.03057 μM
Compound: 14, BC-2059
Growth inhibition of human HCT15 cells after 72 hrs by APH assay
Growth inhibition of human HCT15 cells after 72 hrs by APH assay
[PMID: 26182238]
HCT-15 IC50
0.03806 μM
Compound: 14, BC-2059
Cytotoxicity against human HCT15 cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
Cytotoxicity against human HCT15 cell aggregates grown on matrigel incubated for 72 hrs by MTS assay
[PMID: 26182238]
HT-29 GI50
0.09 μM
Compound: 14, BC-2059
Growth inhibition of human HT-29 cells after 72 hrs by APH assay
Growth inhibition of human HT-29 cells after 72 hrs by APH assay
[PMID: 26182238]
HT-29 IC50
0.63 μM
Compound: 14, BC-2059
Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells assessed as depletion of beta-catenin level by TCF luciferase promoter reporter assay
Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells assessed as depletion of beta-catenin level by TCF luciferase promoter reporter assay
[PMID: 26182238]
MCF7 IC50
0.08078 μM
Compound: 14, BC-2059
Growth inhibition of human MCF7 cells after 72 hrs by APH assay
Growth inhibition of human MCF7 cells after 72 hrs by APH assay
[PMID: 26182238]
SW480 IC50
0.02329 μM
Compound: 14, BC-2059
Growth inhibition of human SW480 cells after 72 hrs by APH assay
Growth inhibition of human SW480 cells after 72 hrs by APH assay
[PMID: 26182238]
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].

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

Tegatrabetan 相关抗体:

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.
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].

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

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.
Clinical Trial
分子量

588.74

Formula

C28H36N4O6S2
CAS 号
性状

固体

颜色

White to light yellow

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
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (84.93 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    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); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    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); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.77%

COA (264 KB) HNMR (297 KB) LCMS (268 KB) 元素分析报告 (210 KB)

产品使用指南 (1538 KB)
参考文献

Tegatrabetan 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6985 mL 8.4927 mL 16.9854 mL 42.4636 mL
5 mM 0.3397 mL 1.6985 mL 3.3971 mL 8.4927 mL
10 mM 0.1699 mL 0.8493 mL 1.6985 mL 4.2464 mL
15 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.8309 mL
20 mM 0.0849 mL 0.4246 mL 0.8493 mL 2.1232 mL
25 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6985 mL
30 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4155 mL
40 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0616 mL
50 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 mL
60 mM 0.0283 mL 0.1415 mL 0.2831 mL 0.7077 mL
80 mM 0.0212 mL 0.1062 mL 0.2123 mL 0.5308 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tegatrabetan1227637-23-1Tegavivint BC2059BC2059BC 2059BC-2059β-cateninBeta cateninInhibitorinhibitorinhibit

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