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Ravoxertinib (GDC-0994)
| Product Name | Ravoxertinib (GDC-0994) |
| Price: | Inquiry |
| Catalog No.: | CN00269 |
| CAS No.: | 1453848-26-4 |
| Molecular Formula: | C21H18ClFN6O2 |
| Molecular Weight: | 439.85 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | OC[C@@H](n1ccc(cc1=O)c1ccnc(n1)Nc1ccnn1C)c1ccc(c(c1)F)Cl |
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| 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. |
| 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. |
| Density | 1.5±0.1 g/cm3 |
| Boiling Point | 734.6±70.0 °C at 760 mmHg |
| 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 |
| Storage condition | -20℃ |