GDC-0994 - Ravoxertinib | RG7842

Based on 41 reference(s) in Google Scholar 8 10 41

Axon 3741

CAS [1453848-26-4]

MF C21H18ClFN6O2
MW 440.86

  • Purity: 99%
  • Optical purity: 99% e.e.
  • Soluble in DMSO



GDC-0994 is an orally available small molecule inhibitor of extracellular signal-regulated kinase 1/2 (ERK1/2), highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively. Daily, oral dosing of GDC-0994 results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. PD biomarker inhibition of phospho-p90RSK in these tumors correlates with potency in vitro and in vivo. In contrast to other published ERK inhibitors, GDC-0994 neither increases nor decreases phospho-ERK, suggesting that different ERK inhibitors have alternative mechanisms of action with respect to feedback signaling. Furthermore, we demonstrate a novel approach for targeting the oncogenic signaling through the RAS pathway by combining ERK and MEK inhibitors.

KEYWORDS: GDC-0994 | Supplier | ERK1/2 inhibitor | Ravoxertinib | RG7842 | GDC0994 | GDC 0994 | RG 7842 | RG-7842 | CT-G0994 | CAS [1453848-26-4] | MAPK | ERK | Inhibitor | Enzymes

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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