product name GDC-0994 (Ravoxertinib)
Description: GDC-0994, also known as ravoxertinib and RG7842, is a potent, orally available ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. It has demonstrated anticancer activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival.
References: J Med Chem. 2016 Jun 23;59(12):5650-60.
439.85
Formula
C21H18ClFN6O2
CAS No.
1453848-26-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 87 mg/mL (197.8 mM)
Water: <1 mg/mL
Ethanol: 87 mg/mL (197.8 mM)
Solubility (In vivo)
2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 30 mg/mL
Synonyms
RG 7842; Ravoxertinib
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19415426
| In Vitro |
In vitro activity: GDC-0994 potently inhibits phospho-p90RSK in tumor cells. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | GDC-0994 (p.o.) results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. In vivo, GDC-0994 (p.o.) inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways, and subsequently prevents ERK-dependent tumor cell proliferation and survival. |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2016 Jun 23;59(12):5650-60. |
