化合物 BC2059|T5642|TargetMol

Tegatrabetan
1227637-23-1

￥532 1mg 起订

￥1230 5mg 起订

￥1960 10mg 起订

上海更新日期：2025-02-28

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 BC2059

英文名称：: Tegatrabetan

CAS号：: 1227637-23-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.18%

产品类别：: 抑制剂

货号：: T5642

Product Introduction

Bioactivity

名称	Tegatrabetan
描述	Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.
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].
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].
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 60 mg/mL (101.91 mM)
关键字	inhibit \| Tegatrabetan \| Inhibitor \| β-catenin \| Beta catenin \| BC 2059 \| BC-2059
相关产品	Urea \| Bisdemethoxycurcumin \| PRI-724 \| Nefopam hydrochloride \| XAV-939 \| EMT inhibitor-1 \| MSAB \| TNIK-IN-3 \| (E)-Ferulic acid \| CHIR-99021 \| Wogonin \| Wnt pathway activator 1
相关库	抑制剂库 \| 神经保护化合物库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 细胞骨架化合物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库 \| 细胞重编程化合物库

BC2059|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务