Network Version
GDC-0623 Data Sheet
| Product Name: | GDC-0623 |
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|---|---|---|
| CAS No.: | 1168091-68-6 | |
| Cat. No.: | HY-15610 | |
| MWt: | 456.21 | |
| Formula: | C16H14FIN4O3 | |
| Purity : | >98% | |
| Solubility: | DMSO : 50 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM). IC50 & Target:Ki: 0.13 nM (MEK1,+ATP) In Vitro:GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF in vitro, and able to block MEK phosphorylation by BRAF(V600E)[1]. GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases[2]. In Vivo:GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models[1]. | ||
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