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GDC-0994 (Ravoxertinib, RG7842)
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).
Catalog NO: CT-G0994
Synonym: Ravoxertinib, RG7842
CAS NO: 1453848-26-4
Mol. Formula: C21H18ClFN6O2
MW: 440.9 (refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material. >99% purity by Achiral and Chiral HPLCs (attached). Hemihydrate, validated by a spot-on Quantitative Elemental Analysis. A pale-yellow crystalline powder. Bulk stock. Prompt.