| Cas No.: | 1453848-26-4 |
| Chemical Name: | Ravoxertinib |
| Synonyms: | GDC-0994;(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;GDC0994;Ravoxertinib;R6AXV96CRH;1-[(1~{s})-1-(4-Chloranyl-3-Fluoranyl-Phenyl)-2-Oxidanyl-Ethyl]-4-[2-[(2-Methylpyrazol-3-Yl)amino]pyrimidin-4-Yl]pyridin-2-One;6QB;1-[(1S)-1-(4-CHLORO-3-FLUOROPHENYL)-2-HYDROXYETHYL]-4-{2-[(2-METHYLPYRAZOL-3-YL)AMINO]PYRIMIDIN-4-YL}PYRIDIN-2-ONE;1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4- |
| SMILES: | O=C1C=C(C2=NC(NC3=CC=NN3C)=NC=C2)C=CN1[C@@H](C4=CC=C(Cl)C(F)=C4)CO |
| Formula: | C21H18ClFN6O2 |
| M.Wt: | 440.858 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively. |
| In Vivo: | In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) is sufficient to achieve the desired target coverage for at least 8 h[1]. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice[2]. |
| In Vitro: | Ravoxertinib (GDC-0994) also inhibits p90RSK with IC50 of 12 nM[1]. Ravoxertinib (GDC-0994) is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2]. |

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