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Background Information:
GDC-0994 (Ravoxertinib, RG7842) 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. GDC-0994 is currently in Phase I clinical development (ref 1).
Reference:
1. K. Robarge, et al, Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA.
APIM050153: GDC-0994 (RAVOXERTINIB, RG7842)
CAS No.: 1453848-26-4.
Molecular Formula: C21H18ClFN6O2.
Molecular Weight: 440.9 (refer to Certificate of Analysis, batch-specific).
Purity: >99.5% chem and optical purity.
QC: HPLC-MS, 1H-NMR, Chiral HPLC, and Quantitative Elemental Analysis report.
Solubility: Refer to Certificate.
Storage: Refer to Certificate.
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