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GDC-0994 is an inhibitor of ERK1/2, which is commonly activated by oncogenic mutations in B-Raf or Ras. It is effective against cancer cell lines that are resistant to B-Raf and MEK1/2 inhibitor therapy. Combination therapy targeting multiple nodes of the Ras/Raf/MEK/ERK signaling cascade enhances efficacy and diminishes the potential for acquired drug resistance.
| Cas No. | 1453848-26-4 |
|---|---|
| Purity | ≥98% |
| Formula | C21H18ClFN6O2 |
| Formula Wt. | 440.86 |
| IUPAC Name | 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one |
| Synonym | GDC0994; RG7842; Ravoxertinib |
| Solubility | Ethanol (30 mg/mL), DMSO (30 mg/mL), DMF (30 mg/mL). |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Roskoski R. Targeting ERK1/2 protein-serine/threonine kinases in human cancers. Pharmacol Res. 142:151-168 (2019). PMID: 30794926.
Blake J., Burkard M., et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development. J Med Chem. 59(12):5650-60 (2016). PMID: 27227380.