| Identification | Back Directory | [Name]
Benzamide, 4-[3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]-2-pyrazinyl]-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluoro-, hydrochloride (1:) | [CAS]
1715025-34-5 | [Synonyms]
Rineterkib HCl
Rineterkib hydrochloride
Benzamide, 4-[3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]-2-pyrazinyl]-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluoro-, hydrochloride (1:) | [Molecular Formula]
C26H28BrClF3N5O2 | [MOL File]
1715025-34-5.mol | [Molecular Weight]
614.89 |
| Hazard Information | Back Directory | [Uses]
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF[1][2]. | [in vivo]
ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the Calu-6 human NSCLC subcutaneous tumor xenograft model in mice[1]. | Animal Model: | Calu-6 NSCLC xenograft tumor models in mice[1]. | | Dosage: | 50, 75 mg/kg. | | Administration: | Orally either daily (qd) or every other day (q2d) for 27 days. | | Result: | Significantly reduced the tumor volume. |
| [storage]
4°C, away from moisture and light | [References]
[1] CAPONIGRO, et al. THERAPEUTIC COMBINATIONS COMPRISING A RAF INHIBITOR AND A ERK INHIBITOR. WO2018051306A1.
[2] Song Y, et al. Targeting RAS-RAF-MEK-ERK signaling pathway in human cancer: current status in clinical trials. Genes & Diseases, 2022. |
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