Tegatrabetan
Based on 6 publication(s) in Google Scholar
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.84%
- No. CAS: 1227637-23-1
- Fòrmula: C28H36N4O6S2
- Peso molecular:588.74
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tegatrabetan
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
Actividad biológica
β-Catenin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.05169 μM
Compound: 14, BC-2059
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Growth inhibition of human A549 cells after 72 hrs by APH assay
Growth inhibition of human A549 cells after 72 hrs by APH assay
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[PMID: 26182238] |
| Cancer cell lines | IC50 |
0.02001 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| Cancer cell lines | IC50 |
0.02075 μM
Compound: 14, BC-2059
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Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay
Cytotoxicity against human prostate cancer cells after 72 hrs by MTS assay
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[PMID: 26182238] |
| Cancer cell lines | IC50 |
0.02992 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| Cancer cell lines | IC50 |
0.5305 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| HCT-116 | IC50 |
0.02019 μM
Compound: 14, BC-2059
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Growth inhibition of human HCT116 cells after 72 hrs by APH assay
Growth inhibition of human HCT116 cells after 72 hrs by APH assay
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[PMID: 26182238] |
| HCT-15 | IC50 |
0.03057 μM
Compound: 14, BC-2059
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Growth inhibition of human HCT15 cells after 72 hrs by APH assay
Growth inhibition of human HCT15 cells after 72 hrs by APH assay
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[PMID: 26182238] |
| HCT-15 | IC50 |
0.03806 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| HT-29 | GI50 |
0.09 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| HT-29 | IC50 |
0.63 μM
Compound: 14, BC-2059
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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
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[PMID: 26182238] |
| MCF7 | IC50 |
0.08078 μM
Compound: 14, BC-2059
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Growth inhibition of human MCF7 cells after 72 hrs by APH assay
Growth inhibition of human MCF7 cells after 72 hrs by APH assay
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[PMID: 26182238] |
| SW480 | IC50 |
0.02329 μM
Compound: 14, BC-2059
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Growth inhibition of human SW480 cells after 72 hrs by APH assay
Growth inhibition of human SW480 cells after 72 hrs by APH assay
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[PMID: 26182238] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60, OCI-AML3 and MV4-11 cells
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Concentration:20, 50, and 100 nM
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Incubation Time:48 hours
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Result:Dose-dependently inhibited cell proliferation.
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Cell Line:OCI-AML3 cells
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Concentration:20 and 50 nM
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Incubation Time:24 hours
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Result:Dose-dependently induced cell cycle growth arrest.
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Cell Line:OCI-AML3, HL-60 and MV4-11 cells
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Concentration:100 nM
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Incubation Time:24 hours
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Result:Treatment depleted β-Catenin expression levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID mice bearing OCI-AML3 xenografts[1]
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Dosage:1 mg/kg; 5 mg/kg; 10 mg/kg
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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.
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Result:Treatment significantly improved survival of NOD/SCID mice bearing OCI-AML3 xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1227637-23-1
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Appearance Solid
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Peso molecular 588.74
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Fòrmula C28H36N4O6S2
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Color White to light yellow
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SMILES
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
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Synonyms
Tegavivint; BC2059
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2025 May 26. PMID: 40419770
Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]
Images of spheroids grown in ultralow attachment plates treated with Tegavivint (Tega) (5 μM), and quantification of spheroid viability was performed with CellTiter-Glo.
Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]
Tegatrabetan (Tega) (10 mg/kg; i.p.; twice a week) enlonged time to tumor tripling of Foxn1nsup>u mouse xenograft tumor model.
Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]
Tegatrabetan (Tega) (2.5 μM) were lethal to RNF43-mutant-HPAF-IIN.
Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]
Tegatrabetan (Tega) (2.5 μM) were lethal to Capan-2 cells.
Tegatrabetan purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 May 26. [Abstract]
Tegavivint (Tega) (10-8-10-5 M; 48 h) caused HT-1080N cell death.
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Eur J Pharmacol
Verdiperstat attenuates acute lung injury by modulating MPO/μ-calpain/β-catenin signaling. [Abstract]2022 Jun 5:924:174940. PMID: 35461824 -
J Cell Sci
Tbl1 promotes Wnt/β-catenin signaling-induced degradation of the Tcf7l1 protein in mouse ESCs. [Abstract]2024 May 1;137(9):jcs261241. PMID: 38639717 -
bioRxiv
2026 Mar 30:2026.03.28.714855. PMID: 41959534 -
bioRxiv
Dyr726, a brain-penetrant inhibitor of PI3Kα, Type III receptor tyrosine kinases, and WNT signaling. [Abstract]2025 Mar 29:2025.03.26.645490. PMID: 40196701 -
Res Sq
2025 Feb 11:rs.3.rs-4138879. PMID: 39989975
Solvente y solubilidad
DMSO : 50 mg/mL (84.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.25 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |
Tegatrabetan Related Classifications
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