CYT387
 | |
| Names | |
|---|---|
| IUPAC name
N-(Cyanomethyl)-4-[2-(4-morpholinoanilino)pyrimidin-4-yl]benzamide | |
| Other names
CYT 11387 | |
| Identifiers | |
| 1056634-68-4 | |
| ChemSpider | 24676202 |
| 7791 | |
| Jmol interactive 3D | Image |
| PubChem | 25062766 |
| |
| |
| Properties | |
| C23H22N6O2 | |
| Molar mass | 414.47 g·mol−1 |
| Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
CYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM).[1]
As of 2011, CYT387 is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for CYT387 include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions.[2]
The drug was originally discovered by Australian drug discovery company Cytopia, then developed by YM BioSciences Inc. (since acquired by Gilead Sciences as of 2013)
References
- ↑ Pardanani, A.; Lasho, T.; Smith, G.; Burns, C. J.; Fantino, E.; Tefferi, A. (2009). "CYT387, a selective JAK1/JAK2 inhibitor: In vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients". Leukemia 23 (8): 1441–1445. doi:10.1038/leu.2009.50. PMID 19295546.
- ↑ Pardanani, A.; Vannucchi, A. M.; Passamonti, F.; Cervantes, F.; Barbui, T.; Tefferi, A. (2010). "JAK inhibitor therapy for myelofibrosis: critical assessment of value and limitations". Leukemia 25 (2): 218–225. doi:10.1038/leu.2010.269. PMID 21079613.
External links
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