For research use only. Not for therapeutic Use.
GDC-0879 (Cat No.:I005410) is a novel and potent, selective B-Raf inhibitor with an IC50 of 0.13 nM in A375 and Colo205 cells, and also inhibits c-Raf; it has no inhibitory effect on other protein kinases.
| Catalog Number | I005410 |
| CAS Number | 905281-76-7 |
| Synonyms | 2-[4-[(1E)-1-hydroxyimino-2,3-dihydroinden-5-yl]-3-pyridin-4-ylpyrazol-1-yl]ethanol |
| Molecular Formula | C19H18N4O2 |
| Purity | ≥95% |
| Target | Raf |
| Solubility | DMSO ≥64mg/mL Water <1.2mg/mL Ethanol ≥4.8mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 0.13 nM [1] |
| Reference | </br>1:Validation and application of a liquid chromatography-tandem mass spectrometric method for the determination of GDC-0879 and its metabolite in dog plasma using solid phase extraction. Chou B, Adler RS, Meng M, Percey S, Dean B, Hop CE, Shin YG.J Pharm Biomed Anal. 2012 Nov;70:354-61. doi: 10.1016/j.jpba.2012.05.029. Epub 2012 Jun 1. PMID: 22717139 </br>2:Disposition of GDC-0879, a B-RAF kinase inhibitor in preclinical species. Choo EF, Driscoll JP, Feng J, Liederer B, Plise E, Randolph N, Shin Y, Wong S, Ran Y.Xenobiotica. 2009 Sep;39(9):700-9. doi: 10.1080/00498250902991827. PMID: 19552528 </br>3:Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression. Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O/’Brien C, Modrusan Z, Seshagiri S, Lackner M, Stern H, Choo E, Murray L, Friedman LS, Belvin M.Cancer Res. 2009 Apr 1;69(7):3042-51. doi: 10.1158/0008-5472.CAN-08-3563. Epub 2009 Mar 10. PMID: 19276360 Free Article</br>4:Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy. Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF.J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. doi: 10.1124/jpet.108.148189. Epub 2009 Jan 15. PMID: 19147858 Free Article |
