| CAS NO: | 1172133-28-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 464.55 |
|---|---|
| Formula | C28H30F2N2O2 |
| CAS No. | 1172133-28-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 13 mg/mL (28.0 mM) |
| Water: <1 mg/mL | |
| Ethanol: 6 mg/mL (12.9 mM) | |
| Other info | Chemical Name: (3E,5E)-3,5-bis(4-fluorobenzylidene)-1-((1-hydroxy-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)methyl)piperidin-4-one InChi Key: PWZQFTQMMAIRRM-JFMUQQRKSA-N InChi Code: InChI=1S/C28H30F2N2O2/c1-27(2)15-23(28(3,4)32(27)34)18-31-16-21(13-19-5-9-24(29)10-6-19)26(33)22(17-31)14-20-7-11-25(30)12-8-20/h5-15,34H,16-18H2,1-4H3/b21-13+,22-14+ SMILES Code: O=C1/C(CN(CC2=CC(C)(C)N(O)C2(C)C)C/C1=C\C3=CC=C(F)C=C3)=C/C4=CC=C(F)C=C4 |
| Synonyms | HO3867; HO 3867; HO-3867 |
| In Vitro | In vitro activity: HO-3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and promotes apoptosis by caspase-8 and caspase-3 activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines. Kinase Assay: HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity. Cell Assay: Cell viability is determined by a colorimetric assay using MTT. In the mitochondria of living cells, yellow MTT undergoes a reductive conversion to formazan, producing a purple color. Cells, grown to ~80% confluence in 75-mm flasks, are trypsinized, counted, seeded in 96-well plates with an average population of 7,000 cells/well, incubated overnight, and then treated with HO-3867 for 24 h. All experiments are done using 8 replicates and repeated at least three times. |
|---|---|
| In Vivo | HO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft tumor in mice without any apparent signs of toxicity, and also results in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting proteins. HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. HO-3867 (100 ppm p.o.) also attenuates left-heart-failure-induced pulmonary hypertension by decreasing oxidative stress and increasing PTEN expression in the lung of rats. |
| Animal model | Mice with ovarian cancer xenograft tumor |
| Formulation & Dosage | 100 ppm p.o. |
| References | Mol Cancer Ther. 2010 May;9(5):1169-79; Cancer Biol Ther. 2011 Nov 1;12(9):837-45. |
m.cnreagent.com