| Identification | Back Directory | [Name]
G-479 | [CAS]
1168092-22-5 | [Synonyms]
G-479
G479; G 479
Imidazo[1,5-a]pyrazine-6-carboxamide, N-[(2R)-2,3-dihydroxypropoxy]-5-[(2-fluoro-4-iodophenyl)amino]- | [Molecular Formula]
C16H15FIN5O4 | [MOL File]
1168092-22-5.mol | [Molecular Weight]
487.22 |
| Hazard Information | Back Directory | [Description]
G-479 is an potent MEK inhibitor. Structurally, G-479 is an analogue of GDC-0623 (or so-call Me-Too drug). G-479 with polarity distributed throughout the molecule was shown improved bioactivity over GDC-0623 in many aspects. | [Uses]
G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats[1]. | [References]
[1] Robarge KD, et al., Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723. DOI:10.1016/j.bmcl.2014.08.008 |
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