HJC-0123
Downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, HJC-0123 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.
1: Chen H, Yang Z, Ding C, Chu L, Zhang Y, Terry K, Liu H, Shen Q, Zhou J. Fragment-based drug design and identification of HJC0123, a novel orally bioavailable STAT3 inhibitor for cancer therapy. Eur J Med Chem. 2013Apr;62:498-507. doi: 10.1016/j.ejmech.2013.01.023. Epub 2013 Jan 26. PubMed PMID: 23416191; PubMed Central PMCID: PMC3750725.
| Chemical | |
|---|---|
| CAS Num | 1430420-02-2 |
| Chemical Formula | C24H16N2O3S |
| Molecular Weight | 412.46 |
| IUPAC Chemical Name | N-(1,1-dioxidobenzo[b]thiophen-6-yl)-2-phenylquinoline-4-carboxamide |
| Exact Mass | 412.08816 |
| Elemental Analysis | C, 69.89; H, 3.91; N, 6.79; O, 11.64; S, 7.77 |
| Synonym | HJC0123; HJC 0123; HJC-0123. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(C1=CC(C2=CC=CC=C2)=NC3=CC=CC=C13)NC4=CC=C(C=CS5(=O)=O)C5=C4 |
| Biological | |
| Targets and Effects | estrogen receptor agonist |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| 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). |
| Shelf Life | >2 years if stored properly |
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