Tegatrabetan

Tegatrabetan is an inhibitor of Wnt/beta-catenin signaling. It reduces Wnt3a-induced transcriptional activity in a reporter activity assay using STF3a cells, which exhibit constitutive Wnt activation, when used at a concentration of 1 µM. Tegatrabetan inhibits proliferation of, and transcription in, HT-29 human colon cancer cells (IC50s = 9 and 63 nM, respectively) and reduces survival in six other cancer cell lines (IC50s = 14-80 nM). It induces cell cycle arrest at the G1 phase in HCT-15 human colon cancer cells when used at a concentration of 625 nM. In vivo, tegatrabetan (50 mg/kg per day) reduces tumor volume and inhibits lung metastasis in a Saos-2 osteosarcoma mouse xenograft model.Formal Name: rel-2,7-bis[[(3R,5S)-3,5-dimethyl-1-piperidinyl]sulfonyl]-9,10-anthracenedione 9,10-dioxime. CAS Number: 1227637-23-1. Synonyms: BC-2059. Molecular Formula: C28H36N4O6S2. Formula Weight: 588.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble. lambdamax: 227, 274, 304 nm. SMILES: ON=C1C2=CC(S(=O)(N3C[C@H](C[C@H](C3)C)C)=O)=CC=C2C(C4=CC=C(S(=O)(N5C[C@H](C[C@H](C5)C)C)=O)C=C41)=NO. 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/t17-,18+,19-,20+. InChi Key: GAPRVZKWPDRAJA-FGYAAKKASA-N.