ERK-IN-1
- Product Name
- ERK-IN-1
- CAS No.
- 1715025-32-3
- Chemical Name
- ERK-IN-1
- Synonyms
- ERK-IN-1;Rineterkib;Rineterkib，LTT-462;Rineterkib(ERK-IN-1;Rineterkib free base;ERK-IN-1 (COMPOUND B);Rineterkib, 10 mM in DMSO;Raf,G12V,Rineterkib,Extracellular signal regulated kinases,G12D,ERK,NSCLC,inhibit,G12C,MAPK,KRAS,Raf kinases,Inhibitor;4-{3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]pyrazin-2-yl}-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluorobenzamide;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-
- CBNumber
- CB15540362
- Molecular Formula
- C26H27BrF3N5O2
- Formula Weight
- 578.42
- MOL File
- 1715025-32-3.mol
ERK-IN-1 Property
- 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)
- pka
- 12.32±0.46(Predicted)
- form
- Solid
- color
- White to light yellow
N-Bromosuccinimide Price
- Product number
- CS-0086360
- Product name
- Rineterkib
- Purity
- 99.21%
- Packaging
- 5mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0086360
- Product name
- Rineterkib
- Purity
- 99.21%
- Packaging
- 10mg
- Price
- $680
- Updated
- 2021/12/16
- Product number
- CS-0086360
- Product name
- Rineterkib
- Purity
- 99.21%
- Packaging
- 25mg
- Price
- $1350
- Updated
- 2021/12/16
ERK-IN-1 Chemical Properties,Usage,Production
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
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.
ERK-IN-1 Preparation Products And Raw materials
Raw materials
Preparation Products
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