iCRT 14

Name	iCRT-14
Synonyms	ICRT14 ICRT-14 CS-1225 iCRT 14 iCRT-14 iCRT 14 (Fandachem) 5-[[2,5-DiMethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]Methylene]-3-phenyl-2,4-thiazolidinedione 2,4-Thiazolidinedione, 5-[[2,5-dimethyl-1-(3-pyridinyl)-1H-pyrrol-3-yl]methylene]-3-phenyl- (5Z)-5-[(2,5-dimethyl-1-pyridin-3-ylpyrrol-3-yl)methylidene]-3-phenyl-1,3-thiazolidine-2,4-dione
CAS	677331-12-3
InChIKey	NCSHZXNGQYSKLR-UNOMPAQXSA-N

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.

Last Update：2024-01-02 23:10:35

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Mobile: 18021002903
QQ: 3008007409

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iCRT 14

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