| Identification | Back Directory | [Name]
ERK-IN-1 | [CAS]
1715025-32-3 | [Synonyms]
ERK-IN-1
Rineterkib
Rineterkib，LTT-462
Rineterkib free base
ERK-IN-1 (COMPOUND B)
Raf,G12V,Rineterkib,Extracellular signal regulated kinases,G12D,ERK,NSCLC,inhibit,G12C,MAPK,KRAS,Raf kinases,Inhibitor | [Molecular Formula]
C26H27BrF3N5O2 | [MDL Number]
MFCD31813792 | [MOL File]
1715025-32-3.mol | [Molecular Weight]
578.42 |
| Chemical Properties | Back Directory | [Boiling point ]
717.6±60.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [solubility ]
DMSO:0.0(Max Conc. mg/mL);0.0(Max Conc. mM) | [form ]
Solid | [pka]
12.32±0.46(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Rineterkib (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]
Rineterkib (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. |
| [IC 50]
ERK1; ERK2; RAF | [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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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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