Tegatrabetan (Synonyms: Tegavivint; BC2059)

Name: Tegatrabetan
Brand: MedChemExpress
SKU: HY-109103
Rating: 4.5 (1 reviews)

Cat. No.: HY-109103 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

For research use only. We do not sell to patients.

Tegatrabetan Chemical Structure

CAS No. : 1227637-23-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 109	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 109	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 473	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 803	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Tegatrabetan

•Eur J Pharmacol. 2022 Apr 21;924:174940. [Abstract]

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References
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Description

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]

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]

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].

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

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.

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].

MedChemExpress (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

Molecular Weight

588.74

Formula

C₂₈H₃₆N₄O₆S₂

CAS No.

1227637-23-1

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.1699 mL	0.8493 mL	1.6985 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (249 KB) HNMR (297 KB) LCMS (268 KB) Elemental Analysis Report (107 KB)

Handling Instructions (2659 KB)

References

[1]. Fiskus W, et al. Pre-clinical efficacy of combined therapy with novel β-catenin antagonist BC2059 and histone deacetylase inhibitor against AML cells. Leukemia. 2015 Jun;29(6):1267-78. [Content Brief]

Complete Stock Solution Preparation Table

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

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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Tegatrabetan (Synonyms: Tegavivint; BC2059)

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Tegatrabetan Related Antibodies

1 Publications Citing Use of MCE Tegatrabetan

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Complete Stock Solution Preparation Table

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