Synonym
BC2059; BC-2059; BC 2059; tegavivint; Tegatrabetan,
IUPAC/Chemical Name
(9E,10E)-2,7-bis(((3R,5S)-3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime
InChi Key
GAPRVZKWPDRAJA-TVRZPQSBSA-N
InChi Code
InChI=1S/C28H36N4O6S2/c1-17-9-18(2)14-31(13-17)39(35,36)21-5-7-23-25(11-21)28(30-34)26-12-22(6-8-24(26)27(23)29-33)40(37,38)32-15-19(3)10-20(4)16-32/h5-8,11-12,17-20,33-34H,9-10,13-16H2,1-4H3/b29-27-,30-28+/t17-,18+,19-,20+
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
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
BC2059 disrupts the WNT/beta-catenin pathway in human tumor cells. In cancer cells, BC2059 potently inhibits the WNT/beta catenin pathway as measured by modulation of clinically relevant target gene expression and a specific decrease in beta catenin protein levels. The mechanism of action for BC2059 is targeted degradation of beta catenin protein in cancer cells followed by reduced expression of beta-catenin-regulated genes that are known to promote and maintain the malignant phenotype. This results in cell cycle arrest and subsequent apoptosis.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
588.74
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Fiskus W, Sharma S, Saha S, Shah B, Devaraj SG, Sun B, Horrigan S, Leveque C, Zu Y, Iyer S, Bhalla KN. Pre-clinical efficacy of combined therapy with novel β-catenin antagonist BC2059 and histone deacetylase inhibitor against AML cells. Leukemia. 2014 Dec 8. doi: 10.1038/leu.2014.340. [Epub ahead of print] PubMed PMID: 25482131.
2: Woo MJ, Choi J, Kang HY, Jang S, Kim MJ, Kim S, Byun S, Jung SK. In Vitro and In Vivo Models for the Development of Hair Growth Materials By Regulating the β-Catenin Signaling Pathways. J Med Food. 2024 May;27(5):449-459. doi: 10.1089/jmf.2023.K.0258. Epub 2024 Feb 29. PMID: 38421731.
