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Tegatrabetan

产品编号 T5642 CAS 1227637-23-1

别名: BC2059

Tegatrabetan (BC2059) 是β-Catenin 拮抗剂，能够破坏 β-catenin 与转导素 β 样蛋白 1 (TBL1) 结合。

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Tegatrabetan, CAS 1227637-23-1

规格	价格/CNY	货期
1 mg	￥ 532	现货
2 mg	￥ 768	现货
5 mg	￥ 1,230	现货
10 mg	￥ 1,960	现货
25 mg	￥ 3,810	现货
50 mg	￥ 5,470	现货
100 mg	￥ 7,670	现货
1 mL * 10 mM (in DMSO)	￥ 1,590	现货

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纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.
体外活性	BC2059 induces apoptosis in primary multiple myeloma samples in vitro, causing minimal apoptosis on healthy peripheral blood mononuclear cells[1].
体内活性	BC2059 synergizes with the proteasome inhibitor bortezomib both in HMCL and primary multiple myeloma samples. Finally, in xenograft models of human myelomatosis, BC2059 delays tumor growth and prolongs survival with minor on-target side effects. Collectively, these results demonstrate the efficacy of targeting the Wnt/β-catenin pathway with BC2059 both in vitro and in vivo, at clinically achievable doses[1].
细胞实验	For β-catenin knockdown, 2 mL of 2 × 10^5/mL KMS18 cells were plated into a 12-well plate at day 0 (KMS18 doubling time: 36 hours).?At day 1, media were replaced by 1 mL of Opti-MEM , and transfection was carried out with Lipofectamine RNAiMAX .?For β-catenin knockdown, we used SignalSilence β-catenin siRNA I and β-catenin siRNA II (Cell Signaling Technology) at concentrations recommended by the manufacturer, whereas Silencer Negative Control No. 1 siRNA ?was used as a negative control, at the same concentration.?Six hours after the transfection, 1 mL of fresh media (RPMI-10% FCS) was added in every well.?At days 2 and 3, cells were treated with BC2059 (50, 100, 150 nmol/L) and then harvested at day 4 (72 hours after transfection).?Cell death was monitored by PI staining with FACS, whereas untreated cells were collected for β-catenin protein level measurement by immunoblotting.?Cells were lysed with RIPA lysis buffer, and 70 μg of protein was separated by 6% SDS-PAGE and blotted onto PVDF as already described.?β-Actin (mouse mAb HRP conjugate;?Cell Signaling Technology) was used as a loading control[1].
动物实验	Adult age-matched Cg-Prkdcscid Il2rgtm1Wjl/SzJ mice were injected (intravenously) with 1 × 10^6 U266 HMCL, carrying the FUL2-TGvector .?At day 21, a limited course of treatment was commenced after confirmation of established measurable disease by bioluminescence.?Control mice (n = 4) received 17% Solutol HS 15 whereas treated mice received 5 (n = 4) or 10 mg/kg BC2059 (n = 5) twice a week intravenously for 3 consecutive weeks (6 doses in total).?Tumor burden was monitored on a weekly basis by in vivo imaging, from the second week of the experiment (day 18) until the first mice reached scientific endpoints.?Briefly, mice were anaesthetized, injected intraperitoneally with 125 mg/kg luciferin, and imaged with the Lumina III XR system.?Acquisition and analysis were performed with the Living Image system.?Peripheral blood counts were evaluated sequentially during the course of the experiment .Upon reaching scientific endpoints (hind limp paralysis, >20% weight loss), mice were humanely euthanized and tissues (skin and colon) were collected.?Tissues were formalin fixed and embedded in paraffin, sectioned, and stained with H&E and β-catenin antibody.?Images were taken with an Olympus BX51 microscope[1].

别名	BC2059
分子量	588.74
分子式	C28H36N4O6S2
CAS No.	1227637-23-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (101.91 mM)

溶液配制表

可选溶剂	浓度体积质量	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
	20 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	50 mM	0.034 mL	0.1699 mL	0.3397 mL	0.8493 mL
	100 mM	0.017 mL	0.0849 mL	0.1699 mL	0.4246 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Savvidou I, Khong T, Cuddihy A, et al. Beta-catenin inhibitor BC2059 is efficacious as monotherapy or in combination with proteasome inhibitor bortezomib in multiple myeloma[J]. Molecular Cancer Therapeutics, 2017, 16(9):molcanther.0624.2016. 2. Fiskus W, Sharma S, Saha S, et al. Pre-clinical efficacy of combined therapy with novel β-catenin antagonist BC2059 and histone deacetylase inhibitor against AML cells[J].Leukemia. 2015 Jun;29(6):1267-78

文献引用

1. Ueda K, Kumari R, Schwenger E, et al. MDMX acts as a pervasive preleukemic-to-acute myeloid leukemia transition mechanism. Cancer cell. 2021, 39(4): 529-547. e7.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tegatrabetan 1227637-23-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin inhibit Inhibitor BC2059 β-catenin Beta catenin BC 2059 BC-2059 inhibitor

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Tegatrabetan

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords