WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205772
Description: GDC-0623, also known as G-868, is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
MedKoo Cat#: 205772
Chemical Formula: C16H14FIN4O3
Exact Mass: 456.00946
Molecular Weight: 456.21
Elemental Analysis: C, 42.12; H, 3.09; F, 4.16; I, 27.82; N, 12.28; O, 10.52
Synonym: GDC0623; GDC-0632; GDC 0632; G868; G 868; G-868.
IUPAC/Chemical Name: 5-((2-fluoro-4-iodophenyl)amino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide
InChi Key: RFWVETIZUQEJEF-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H14FIN4O3/c17-13-7-10(18)1-4-14(13)20-15-12(16(24)21-25-6-5-23)3-2-11-8-19-9-22(11)15/h1-4,7-9,20,23H,5-6H2,(H,21,24)
SMILES Code: O=C(C1=C(NC2=CC=C(I)C=C2F)N3C(C=C1)=CN=C3)NOCCO
GDC-0623, a selective inhibitor of MEK, also known as mitogen activated protein kinase kinase (MAPKK), is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. Inappropriate activation of the MEK/ERK pathway promotes cell growth in the absence of exogenous growth factors.
G479 is Me-Too version of GDC-0623. Their structures are shown below (side-by-side comparison)
G479 is Me-Too version
of GDC-0623. Their structures are shown below (side-by-side comparison)
1: Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M. 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):4714-23. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15. PubMed PMID: 25193232.
2: Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Erratum in: Nature. 2013 Oct 10;502(7470):258. PubMed PMID: 23934108.