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Tegatrabetan

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Catalog No. T5642Cas No. 1227637-23-1
Alias BC2059

Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.

Tegatrabetan

Tegatrabetan

🥰Excellent
Purity: 99.18%
Catalog No. T5642Alias BC2059Cas No. 1227637-23-1
Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.
Pack SizePriceAvailabilityQuantity
1 mg$34In Stock
2 mg$48In Stock
5 mg$77In Stock
10 mg$126In Stock
25 mg$220In Stock
50 mg$352In Stock
100 mg$595In Stock
1 mL x 10 mM (in DMSO)$88In Stock
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Purity:99.18%
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Product Introduction

Bioactivity
Description
Tegatrabetan (BC2059) is a small molecule inhibitor of the Wnt/beta-catenin pathway with potential antineoplastic activity.
In vitro
BC2059 induces apoptosis in primary multiple myeloma samples in vitro, causing minimal apoptosis on healthy peripheral blood mononuclear cells[1].
In vivo
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].
Cell Research
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].
Animal Research
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].
AliasBC2059
Chemical Properties
Molecular Weight588.74
FormulaC28H36N4O6S2
Cas No.1227637-23-1
SmilesC[C@H]1C[C@@H](C)CN(C1)S(=O)(=O)c1ccc2C(=NO)c3ccc(cc3C(=NO)c2c1)S(=O)(=O)N1C[C@@H](C)C[C@@H](C)C1
Relative Density.1.46 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/mL (101.91 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6985 mL8.4927 mL16.9854 mL84.9271 mL
5 mM0.3397 mL1.6985 mL3.3971 mL16.9854 mL
10 mM0.1699 mL0.8493 mL1.6985 mL8.4927 mL
20 mM0.0849 mL0.4246 mL0.8493 mL4.2464 mL
50 mM0.0340 mL0.1699 mL0.3397 mL1.6985 mL
100 mM0.0170 mL0.0849 mL0.1699 mL0.8493 mL

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