ICG-001

2 years -80 in solvent

Water-soluble analog of ICG-001 is treated orally for 9 weeks everyday.

Human colon carcinoma cell lines SW480, SW620, and HCT116, normal colonic epithelial cell line CCD-841Co

300 mg/kg

3 uM, [1], 3 uM, [1], 3 uM, [1], 3 uM, [1], 3 uM, [1], 3 uM, [1]

Administration of a water-soluble analog of ICG-001 for 9 weeks reduces the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent Sulindac, which has consistently demonstrated efficacy in this model. No overt toxicity is detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of analog demonstrates a dramatic reduction in tumor volume over the 19-day course of treatment, with no mortality or weight loss. [1] ICG-001 (5 mg/kg per day) significantly inhibits beta-catenin signaling and attenuates bleomycin-induced lung fibrosis in mice, while concurrently preserving the epithelium. [4]

DUAL-Luciferase Reporter Assay, The Dual-Luciferase Reporter (DLR) Assay System provides an efficient means of performing dual reporter assays. In the DLRTM Assay, the activities of firefly (Photinus pyralis) and Renilla (Renilla reniformis, also known as sea pansy) luciferases are measured sequentially from a single sample. The firefly luciferase reporter is measured first by adding Luciferase Assay Reagent II (LAR II) to generate a “glow-type†luminescent signal. After quantifying the firefly luminescence, this reaction is quenched, and the Renilla luciferase reaction is initiated by simultaneously adding Stop & Glo Reagent to the same tube. The Stop & Glo Reagent also produces a “glow-type†signal from the Renilla luciferase, which decays slowly over the course of the measurement. In the DLRTM Assay System, both reporters yield linear assays with subattomole (<10-18) sensitivities and no endogenous activity of either reporter in the experimental host cells. Furthermore, the integrated format of t Assay provides rapid quantitation of both reporters either in transfected cells or in cell-free transcription/translation reactions.

DMSO 110 mg/mL, Water <1 mg/mL, Ethanol 45 mg/mL

(6S, 9aS)-6-(4-hydroxybenzyl)-N-benzyl-8-(naphthalen-1-ylmethyl)-4, 7-dioxo-hexahydro-2H-pyrazino[1, 2-a]pyrimidine-1(6H)-carboxamide