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Purity: ≥98%
Tegatrabetan(also known as Tegavivint; BC-2059; BC 2059; BC2059) is an orally bioavailable and potent β-catenin inhibitor with potential anticancer activity. BC2059 potently induces apoptosis as a single agent and in combination with bortezomib in multiple myeloma. BC2059 induced apoptosis in 10/10 genetically heterogeneous human myeloma cell lines (HMCL) treated with dosages ranging from 50-500nM.
| ln Vitro |
Tegatrabetan (BC2059; 20-100 nM; 48 hours) promotes dose-dependent apoptosis in cultured human acute myeloid leukemia (AML) HL-60, OCI-AML3, and MV4-11 cells and suppresses cell proliferation in suspension culture for more than 120 hours [1]. Tegatrabetan (20 and 50 nM; 24 hours) causes the cell cycle's G2/M phase to diminish concurrently with a minor but considerable accumulation of cells in the G0/G1 phase [1]. In OCI-AML3, HL-60, and MV4-11 cells, tegatrabetan (100 nM, 24 hours) reduces β-catenin levels and its target genes, such as c-MYC and survivin, without changing TBL1 levels [1].
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| ln Vivo |
The median survival of mice treated intravenously with tatetrabetan (BC2059; 1.0 or 5.0 mg/kg/day) increased dramatically from about 17.5 days to 39 days. Intravenous Tegatrabetan (10 mg/kg/day) treatment was the only way to increase median survival to 51.5 days [1].
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: HL-60, OCI-AML3 and MV4-11 Cell Tested Concentrations: 20, 50 and 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: Dose-dependent inhibition of cell proliferation. Cell cycle analysis[1] Cell Types: OCI-AML3 Cell Tested Concentrations: 20 and 50 nM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent induction of cell cycle growth arrest. Western Blot Analysis[1] Cell Types: OCI-AML3, HL-60 and MV4-11 Cell Tested Concentrations: 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Treatment diminished β-Catenin expression levels. |
| Animal Protocol |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse bearing OCI-AML3 xenografts [1]
Doses: 1 mg/kg; 5 mg/kg; 10 mg/kg Route of Administration: intravenous (iv) (iv)injection; 1 mg/kg daily, weekly 4 days, either 5 mg/kg or 10 mg/kg BC2059 twice weekly (Tuesday and Thursday) for 3 weeks. Experimental Results: Treatment Dramatically improved survival of NOD/SCID (severe combined immunodeficient) mouse carrying OCI-AML3 xenografts. |
| 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.
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| Molecular Formula |
C28H36N4O6S2
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|---|---|
| Molecular Weight |
588.7386
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| CAS # |
1227637-23-1
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| Related CAS # |
1227637-23-1
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| SMILES |
S(C1C=CC2C(=C3C=CC(=CC3=C(C=2C=1)N=O)S(N1C[C@H](C)C[C@H](C)C1)(=O)=O)NO)(N1C[C@H](C)C[C@H](C)C1)(=O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~84.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.25 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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