Ravoxertinib
Modify Date: 2024-01-02 18:21:16
Ravoxertinib structure
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Common Name | Ravoxertinib | ||
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| CAS Number | 1453848-26-4 | Molecular Weight | 440.858 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 734.6±70.0 °C at 760 mmHg | |
| Molecular Formula | C21H18ClFN6O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 398.0±35.7 °C | |
Use of RavoxertinibRavoxertinib (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. |
| Name | (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 |
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| Synonym | More Synonyms |
| 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. |
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| Related Catalog | |
| Target |
ERK1:6.1 nM (IC50) ERK2:3.1 nM (IC50) p-RSK:12 nM (IC50) |
| 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]. |
| 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]. |
| Animal Admin | Mice[1] PK/PD data for Ravoxertinib (GDC-0994) in the HCT116 mouse xenograft model. HCT116 tumors are established in nude mice to a tumor volume of 400-600 mm3. Mice are treated with a single oral dose of 22 at 15, 30, or 100 mg/kg versus vehicle control alone (40% PEG400/60% (10% HPβCD)) follow by tumor and plasma collection at 2, 8, 16, and 24 h postdose. Tumor levels of phosphorylated p90RSK (pRSK) relative total p90RSK (tRSK) are measured by quantitative Western blot and are normalized to vehicle control at 2 h postdose (set to 100%). Plasma and tumor concentrations are measured by LC−MS. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 734.6±70.0 °C at 760 mmHg |
| Molecular Formula | C21H18ClFN6O2 |
| Molecular Weight | 440.858 |
| Flash Point | 398.0±35.7 °C |
| Exact Mass | 440.116394 |
| PSA | 97.86000 |
| LogP | 2.18 |
| Vapour Pressure | 0.0±2.5 mmHg at 25°C |
| Index of Refraction | 1.687 |
| Storage condition | -20℃ |
| gdc-0994 |
| gdc0994 |
| 1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-{2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl}-2(1H)-pyridinone |
| 2(1H)-Pyridinone, 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]- |