货号:A503122
同义名:
BC2059; Tegavivint
Tegatrabetan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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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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|---|---|---|---|---|---|---|---|
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| 描述 | β-Catenin (Armadillo in Drosophila) is a multitasking and evolutionary conserved molecule that in metazoans exerts a crucial role in a multitude of developmental and homeostatic processes. More specifically, β-catenin is an integral structural component of cadherin-based adherens junctions, and the key nuclear effector of canonical Wnt signalling in the nucleus[3]. BC2059 is a potent inhibitor of β-Catenin. BC2059 attenuates β-catenin levels, in both the cytoplasm and the nucleus, reducing the transcriptional activity of the TCF4/LEF complex and the expression of its target gene axin 2. Treatment of HMCL (human myeloma cell lines) with BC2059 inhibits proliferation and induces apoptosis in a dose-dependent manner. This is also observed in HMCL-stromal cell cocultures, mitigating the protective effect afforded by the stroma. Similarly, BC2059 induces apoptosis in primary multiple myeloma samples in vitro, causing minimal apoptosis on healthy peripheral blood mononuclear cells[4]. BC2059 treatment disrupted the binding of β-catenin with the scaffold protein transducin β-like 1 and proteasomal degradation and decline in the nuclear levels of β-catenin. BC2059 treatment dose-dependently induced apoptosis of cultured and primary AML BPCs (acute myeloid leukemia blast progenitor cells). Treatment with BC2059 also significantly improved the median survival of immune-depleted mice engrafted with either cultured or primary AML BPCs, exhibiting nuclear expression of β-catenin[5]. In xenograft models of human myelomatosis, BC2059 delayed tumor growth and prolonged survival with minor on-target side effects. These findings support further clinical evaluation of BC2059 for the treatment of multiple myeloma[4]. |
| Concentration | Treated Time | Description | References | |
| hFOB1.19 | > 1 µM | 72 h | hFOB1.19 cells were not sensitive to Tegavivint | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| MV4-11 cells | 20-100 nM | 48 h | BC2059 induced apoptosis in FLT3-ITD expressing MV4-11 cells | Leukemia. 2015 Jun;29(6):1267-78. |
| DLBCL cell lines | 2-100 nM | 24 h | induced DLBCL cell death | Haematologica. 2021 Nov 1;106(11):2927-2939. |
| TCCC-OS84 | 21.6 nM | 72 h | TCCC-OS84 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| TCCC-OS63 | 36.6 nM | 72 h | TCCC-OS63 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| LM7 | 18.0 nM | 72 h | LM7 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| SaOS-2 | 6.2 nM | 72 h | SaOS-2 cells were sensitive to Tegavivint, and it inhibited the expression of b-catenin and c-Myc | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| BCPAP cells | 100 nM | 24 h | Tegavivint significantly reversed the impact of CDH4 on tube formation in HUVECs. | J Transl Med. 2024 Feb 24;22(1):201. |
| TPC-1 cells | 100 nM | 24 h | Tegavivint effectively counteracted the pro-migratory and invasive effects of CDH4 on PTC cells. | J Transl Med. 2024 Feb 24;22(1):201. |
| CD34+ AML blast progenitor cells | 20-100 nM | 48 h | BC2059 dose-dependently induced apoptosis in CD34+ AML blast progenitor cells | Leukemia. 2015 Jun;29(6):1267-78. |
| OCI-AML3 cells | 20-100 nM | 120 h | BC2059 dose-dependently inhibited cell proliferation and induced apoptosis | Leukemia. 2015 Jun;29(6):1267-78. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Osteosarcoma PDX model | Intraperitoneal injection | 50 mg/kg | Twice weekly for 4 weeks | Tegavivint significantly suppressed PDX tumor growth and reduced lung metastasis | J Natl Cancer Inst. 2019 Nov 1;111(11):1216-1227. |
| Nude mice | Lung metastatic model and tumorigenicity studies | Intraperitoneal injections | 20 mg/kg | Twice weekly for three consecutive weeks per cycle, repeated over two cycles lasting 28 days each | Tegavivint significantly impeded tumor formation in CDH4-overexpressing TPC-1 cells and significantly reduced the volume and weight of tumors compared to both control and CDH4-overexpressing groups. | J Transl Med. 2024 Feb 24;22(1):201. |
| NOD/SCID mice | AML xenograft model | Tail vein injection | 1.0, 5.0, 10.0 mg/kg | Twice weekly for 3 weeks | BC2059 significantly improved the survival of NOD/SCID mice | Leukemia. 2015 Jun;29(6):1267-78. |
| NSG mice | DLBCL models | Tail vein injection | 25 mg/kg | Every 3 days until the end of the experiment | Significantly prolonged survival | Haematologica. 2021 Nov 1;106(11):2927-2939. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.70mL 0.34mL 0.17mL |
8.49mL 1.70mL 0.85mL |
16.99mL 3.40mL 1.70mL |
|
| CAS号 | 1227637-23-1 |
| 分子式 | C28H36N4O6S2 |
| 分子量 | 588.74 |
| SMILES Code | O=S(C1=CC2=C(C=C1)/C(C3=CC=C(S(=O)(N4C[C@H](C)C[C@H](C)C4)=O)C=C3/C2=N\O)=N\O)(N5C[C@H](C)C[C@H](C)C5)=O |
| MDL No. | MFCD32633578 |
| 别名 | BC2059; Tegavivint |
| 运输 | 蓝冰 |
| InChI Key | OMWCXCBGEFHCTN-FGYAAKKASA-N |
| Pubchem ID | 46212391 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(84.93 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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