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1168091-68-6O=C(NOCCO)c1ccc2cncn2c1Nc1ccc(I)cc1FRFWVETIZUQEJEF-UHFFFAOYSA-NGDC-0623 is a member of the class of imidazopyridines that is imidazo[1,5-a]pyridine substituted by (2-fluoro-4-iodophenyl)amino and (2-hydroxyethoxy)aminoacyl groups at positions 5 and 6. It is a potent ATP non-competitive inhibitor of MEK1 (Ki = 0.13nM) and also has efficacy against both mutant BRAF and mutant KRAS. It is in clinical development for treatment of patients with locally advanced or metastatic solid tumors. It has a role as an antineoplastic agent, an apoptosis inducer and an EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor. It is a primary alcohol, an organoiodine compound, an imidazopyridine, a substituted aniline, a secondary amino compound, a hydroxamic acid ester and a member of monofluorobenzenes.
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BeschreibungGDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki = 0.13 nM in the presence of ATP). It inhibits the proliferation of A375 BRAF(V600E) and HCT116 KRAS(G13D)-mutant cancer cell lines with EC50 values of 7 and 42 nM, respectively. GDC-0623 inhibits ERK and BIM phosphorylation resulting in upregulation and stabilization of pro-apoptotic BIM protein in KRAS mutant and wild-type HCT116 cells and in KRAS mutant GW620 cells.
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1168091-68-6CHEMBL3330650CHEBI:167659