Molecular Formula | C21H17N3O2S |
Molar Mass | 375.44 |
Density | 1.29±0.1 g/cm3(Predicted) |
Melting Point | 183-186°C |
Boling Point | 567.0±60.0 °C(Predicted) |
Solubility | DMSO: ≥10mg/mL |
Appearance | powder |
Color | yellow to orange |
pKa | 2.09±0.12(Predicted) |
Storage Condition | 2-8°C |
In vitro study | iCRT14 inhibits the transcriptional activity of canonical Wnt signaling, down-regulates Wnt/β-catenin-induced target genes, and inhibits the growth of colorectal cancer cells in vivo. iCRT14 can appropriately reduce Dvl without affecting the phosphorylation of Dvl. In mammalian HEK293 cells, iCRT14 inhibited the Wnt response element STF16-luc reporter gene with an IC50 of 40.3 nM. In addition to affecting the interaction of TCF-β-catenin, iCRT14 can also interfere with the binding of TCF to DNA. |
In vivo study | In the HCT116 and HT29 xenograft models, iCRT14 can cause a significant decrease in CycD1 and a decrease in tumor proliferation. In addition, the initial growth rate of the tumor decreased significantly during the first three weeks of dosing. After 19 days of administration, the tumor growth rate returned to the level of the control group. The mice did not have any symptoms of systemic toxic effects or weight loss during the course of the study. The modified compound can be rapidly metabolized in vivo, and its bioavailability is low. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.664 ml | 13.318 ml | 26.635 ml |
5 mM | 0.533 ml | 2.664 ml | 5.327 ml |
10 mM | 0.266 ml | 1.332 ml | 2.664 ml |
5 mM | 0.053 ml | 0.266 ml | 0.533 ml |